AHR antagonist 5 free base

发表于2024年10月28日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AHR antagonist 5 free base

AHR antagonist 5 free base 是一种选择性的、具有口服活性的芳烃受体 (AHR) 抑制剂。AHR antagonist 5 free base 有效阻止 AHR 从细胞质转移到细胞核。AHR antagonist 5 free base 对 AHR 的选择性高于其他受体、转运蛋白和激酶，并具有抗癌作用。

AHR antagonist 5 free base Chemical Structure

CAS No. : 2247950-42-9

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10 mg	￥8500	询问价格 & 货期

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生物活性	AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases^[1].
体外研究 (In Vitro)	AHR antagonist 5 free base (Compound A) potently inhibits AHR activity in human and rodent cell lines (IC₅₀ of ~35-150 nM). In human T cell assays, AHR antagonist 5 free base induces an activated T cell state. AHR antagonist 5 free base inhibits CYP1A1 and interleukin (IL)-22 gene expression and leads to an increase in pro-inflammatory cytokines, such as IL-2 and IL-9^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)	AHR antagonist 5 free base (Compound A) has been evaluated in a series of pharmacological, single-dose and repeated-dose toxicological studies in rodent and non-rodent species including 28-day Good Laboratory Practice (GLP) studies in rat and monkeys. All changes are resolved or resolving after 2 weeks of dosing cessation, except for the testicular changes in rats^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	441.50
Formula	C₂₅H₂₄FN₇
CAS 号	2247950-42-9
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Marta Sanchez-Martin, et al. Ahr inhibitors and uses thereof. WO2021142180A1.

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CCR4 antagonist 3 hydrochloride

发表于2024年10月28日由上海金畔生物科技有限公司

CCR4 antagonist 3 hydrochloride 纯度: 98.59%

CCR4 antagonist 3 hydrochloride 是口服有效和选择性的 CCR4 拮抗剂。CCR4 antagonist 3 具有新颖的哌啶基-氮杂环丁烷基序，在钙流量和 CTX 分析中的 IC₅₀ 为 22 nM 和 50 nM。CCR4 antagonist 3 具有抗肿瘤活性。

CCR4 antagonist 3 hydrochloride Chemical Structure

CAS No. : 2174938-71-5

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CCR4 antagonist 3 hydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC₅₀s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity^[1].

IC₅₀ & Target

CCR4

体外研究
(In Vitro)

CCR4 antagonist 3 (compound 38) shows no activity in a CYP450 induction assay^[1].
CCR4 antagonist 3 inhibits the migration of mouse iT_reg cells with an IC₅₀ of 39 nM, while the IC₅₀ in human iT_reg cells is 33 nM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CCR4 antagonist 3 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth^[1].
CCR4 antagonist 3 (0.5 mg/kg; IV) has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse^[1].
CCR4 antagonist 3 has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4 antagonist 3 has low clearance (CL=3.7 mL/min/kg), a long terminal half-life (10.7 hr), and good bioavailability (%F = 41) in cynomolgus monkey^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor^[1]
Dosage:	50 mg/kg
Administration:	PO; daily; for 40 days
Result:	Significantly reduced the tumor growth.

Animal Model:	Rat and mouse^[1]
Dosage:	0.5 mg/kg of IV; 2 mg/kg of PO
Administration:	IV or PO
Result:	Possessed medium clearance (CL=47.6 mL/min/kg) and was 49% bioavailable upon oral dosing in rat. Had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

Formula

C₂₄H₂₇C_l2N₇O.xHCl

CAS 号

2174938-71-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 170 mg/mL (Need ultrasonic)

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 4.25 mg/mL (Infinity mM); Clear solution

此方案可获得 ≥ 4.25 mg/mL (Infinity mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 42.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 4.25 mg/mL (Infinity mM); Clear solution

此方案可获得 ≥ 4.25 mg/mL (Infinity mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 42.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Omar Robles, et al. Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as Single Agent and in Combination with Checkpoint Inhibitors. J Med Chem. 2020 Jul 15.

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Antagonist G

发表于2024年10月10日由上海金畔生物科技有限公司

Antagonist G 纯度: 95.0%

Antagonist G 是有效的后叶加压素 (vasopressin) 的拮抗剂。Antagonist G 也是弱的 GRP 和缓激肽的弱拮抗剂。Antagonist G 可诱导 AG-1 的转录，是癌细胞对化疗增敏。

Antagonist G Chemical Structure

CAS No. : 115150-59-9

规格	价格	是否有货
1 mg	￥1500	In-stock
5 mg	￥4500	In-stock
10 mg		询价
50 mg		询价

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生物活性

Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy^[1]^[2].

体外研究
(In Vitro)

Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells^[2].
Antagonist G activates JNK1 in SCLC cells^[2].
Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells.
Concentration:	0-100 μM.
Incubation Time:	24 h.
Result:	Inhibited cell growh.

分子量

951.19

Formula

C₄₉H₆₆N₁₂O₆S

CAS 号

115150-59-9

Sequence Shortening

RW-{Me-Phe}-WLM-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

H₂O

Peptide Solubility and Storage Guidelines:

1. Calculate the length of the peptide.

2. Calculate the overall charge of the entire peptide according to the following table:

	Contents	Assign value
Acidic amino acid	Asp (D), Glu (E), and the C-terminal -COOH.	-1
Basic amino acid	Arg (R), Lys (K), His (H), and the N-terminal -NH₂	+1
Neutral amino acid	Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)	0

3. Recommended solution:

Overall charge of peptide	Details
Negative (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0)	1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)	1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

参考文献

[1]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73.

[2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948.

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Bcl-xL antagonist 2

发表于2024年9月28日由上海金畔生物科技有限公司

Bcl-xL antagonist 2 纯度: 98.46%

Bcl-xL antagonist 2 是一种有效的，选择性的，并具有口服活性的 BCL-X_L 拮抗剂。IC₅₀ 和 K_i 值分别为 0.091 μM和 65 nM。Bcl-xL antagonist 2 可以促进癌细胞凋亡 (apoptosis)。Bcl-xL antagonist 2 有针对研究慢性淋巴细胞白血病 (CLL) 和非霍奇金淋巴瘤 (NHL) 的潜力。

Bcl-xL antagonist 2 Chemical Structure

CAS No. : 1235032-75-3

规格	价格	是否有货
5 mg	￥4500	In-stock
10 mg	￥8000	In-stock
50 mg		询价
100 mg		询价

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Bcl-xL antagonist 2 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Anti-Blood Cancer Compound Library

生物活性

Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-X_L with an IC₅₀ and K_i of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL)^[1]^[2].

IC₅₀ & Target

0.091 μM (BCL-X_L)^[1]

体内研究
(In Vivo)

Assessment of Pharmacokinetics (PK) profile of Bcl-xL antagonist 2 (compound 14) in rat^[1].

iv (1 mg/kg)			po (5 mg/kg)
CL_p (mL/min/kg)	V_ss (L/kg)	t 1/2 (h)	F %
0.47	0.16	6.0	16

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

436.51

Formula

C₂₁H₁₆N₄O₃S₂

CAS 号

1235032-75-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (143.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2909 mL	11.4545 mL	22.9090 mL
5 mM	0.4582 mL	2.2909 mL	4.5818 mL
10 mM	0.2291 mL	1.1454 mL	2.2909 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 6.25 mg/mL (14.32 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (14.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Koehler MF, et al. Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL. ACS Med Chem Lett. 2014;5(6):662-667.

[2]. Wang L, et al. Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor. ACS Med Chem Lett. 2020;11(10):1829-1836.

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R-7050(Synonyms: TNF-α Antagonist III)

发表于2024年9月15日由上海金畔生物科技有限公司

R-7050 (Synonyms: TNF-α Antagonist III) 纯度: 99.26%

R-7050 (TNF-α Antagonist III) 是一种肿瘤坏死因子受体 (TNFR) 拮抗剂，对 TNFα 具有更高选择性。

R-7050 Chemical Structure

CAS No. : 303997-35-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥847	In-stock
5 mg	￥770	In-stock
10 mg	￥1350	In-stock
25 mg	￥2700	In-stock
50 mg	￥4700	In-stock
100 mg	￥8200	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

R-7050 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Pyroptosis Compound Library
Angiogenesis Related Compound Library
Targeted Diversity Library

生物活性

R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.

IC₅₀ & Target^[1]

TNFα

体外研究
(In Vitro)

R-7050 (TNF-α Antagonist III) is a potent and fully reversible hit with greater selectivity toward TNFα. In TNFα-induced intercellular adhesion molecule 1 (ICAM-1) expression, R-7050 inhibition potency (EC₅₀=0.63 μM) is 2- to 3-fold greater than EC₅₀ for IL-1β-induced ICAM-1 expression (EC₅₀=1.45 2 μM). R-7050 inhibits phosphorylation of both the JNK pathway (MKK4, JNKs, and ATF2) and p38 pathway (MKK3/6, p38, and MAPKAP2)^[1]. R-7050 is a cell-permeable triazoloquinoxaline compound that selectively inhibits TNF-α induced cellular signaling. Unlike biologic TNF inhibitors (e.g. Infliximab, Etanercept, Adalimumab) that directly bind TNF-α and function as decoy receptors, R-7050 does not affect binding of TNF-α to TNFR. In contrast, R-7050 selectively inhibits the association of TNFR with intracellular adaptor molecules (e.g. TRADD, RIP), limits receptor internalization, and prevents subsequent cellular responses after TNF-α binding^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

R-7050 (TNF-α Antagonist III) (6 mg/kg) reduces Evans blue extravasation to 28.7±5.9 μg and 30.3±1.9 μg Evans blue/g brain tissue when administered at 0.5 h or 2 h post-ICH, respectively (p<0.05 and p<0.01 vs ICH, respectively; not significantly different from sham). Brain water content, a measure of brain edema, increases from 75.6±0.3% in sham-operated mice to 81.5±0.5% at 24h post-ICH (p<0.05 vs. sham). 6, 12, or 18 mg/kg R-7050 reduces brain water content to 78.5±0.3%, 78.3±0.3%, or 79.3±0.5%, respectively (all treatments p<0.05 vs. ICH; treatments not significantly different from each other). Notably, mice treated with 18 mg/kg exhibit a reduction in general activity/locomotion. As is observed with Evans blue extravasation, R-7050 (6 mg/kg) significantly reduces brain water content after ICH. Administration of R-7050 at 0.5h or 2h post-ICH attenuates brain water content to levels observed in sham-operated mice (p<0.05 vs ICH, not significantly different from sham)^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

380.77

Formula

C₁₆H₈ClF₃N₄S

CAS 号

303997-35-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL (65.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6263 mL	13.1313 mL	26.2626 mL
5 mM	0.5253 mL	2.6263 mL	5.2525 mL
10 mM	0.2626 mL	1.3131 mL	2.6263 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 2.5 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.57 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.57 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.57 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Gururaja TL, et al. A class of small molecules that inhibit TNFalpha-induced survival and death pathways viaprevention of interactions between TNFalphaRI, TRADD, and RIP1. Chem Biol. 2007 Oct;14(10):1105-18.

[2]. King MD, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebralhemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6.

Animal Administration ^[2]	Mice^[2] A mouse collagenase model of ICH is utilized. Briefly, male CD-1 mice (8-10 weeks old) are placed into a stereotactic frame and a 0.5 mm diameter burr hole is drilled over the parietal cortex, 2.2 mm lateral to the bregma. A 26-gauge Hamilton syringe, loaded with 0.04 U of bacterial type IV collagenase in 0.5 μL saline, is lowered 3 mm deep from the skull surface directly into the left striatum. The syringe is depressed at a rate of 450 nL/min and left in place for several minutes after the procedure to prevent solution reflux and excess diffusion. Sham animals undergo the same surgical procedure, except that saline is stereotactically injected rather than collagenase. After the syringe is removed, bone wax is used to close the burr hole, the incision is surgically stapled, and mice are kept warm until recovery of the righting reflex. R-7050 (6-18 mg/kg) is administered via intraperitoneal route at the time of injury or up to 2 h post-ICH^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Gururaja TL, et al. A class of small molecules that inhibit TNFalpha-induced survival and death pathways viaprevention of interactions between TNFalphaRI, TRADD, and RIP1. Chem Biol. 2007 Oct;14(10):1105-18. [2]. King MD, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebralhemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6.

Animal Administration
^[2]

Mice^[2]
A mouse collagenase model of ICH is utilized. Briefly, male CD-1 mice (8-10 weeks old) are placed into a stereotactic frame and a 0.5 mm diameter burr hole is drilled over the parietal cortex, 2.2 mm lateral to the bregma. A 26-gauge Hamilton syringe, loaded with 0.04 U of bacterial type IV collagenase in 0.5 μL saline, is lowered 3 mm deep from the skull surface directly into the left striatum. The syringe is depressed at a rate of 450 nL/min and left in place for several minutes after the procedure to prevent solution reflux and excess diffusion. Sham animals undergo the same surgical procedure, except that saline is stereotactically injected rather than collagenase. After the syringe is removed, bone wax is used to close the burr hole, the incision is surgically stapled, and mice are kept warm until recovery of the righting reflex. R-7050 (6-18 mg/kg) is administered via intraperitoneal route at the time of injury or up to 2 h post-ICH^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Gururaja TL, et al. A class of small molecules that inhibit TNFalpha-induced survival and death pathways viaprevention of interactions between TNFalphaRI, TRADD, and RIP1. Chem Biol. 2007 Oct;14(10):1105-18.

[2]. King MD, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebralhemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6.

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AR antagonist 1

发表于2024年8月13日由上海金畔生物科技有限公司

AR antagonist 1

AR antagonist 1 (compound 29) 是一种有效的 AR 拮抗剂，与 E3 连接酶配体结合，与 VHL 蛋白结合亲和力较弱，用于合成PROTAC ARD-266 (HY-133020)。

AR antagonist 1 Chemical Structure

CAS No. : 1818885-54-9

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生物活性	AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
IC₅₀ & Target	IC50: androgen receptor^[1]
体外研究 (In Vitro)	AR antagonist 1 (compound 29) is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	278.78
Formula	C₁₅H₁₉ClN₂O
CAS 号	1818885-54-9
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231.

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CCR4 antagonist 3

发表于2024年8月11日由上海金畔生物科技有限公司

CCR4 antagonist 3

CCR4 antagonist 3 是口服有效和选择性的 CCR4 拮抗剂。CCR4 antagonist 3 具有新颖的哌啶基-氮杂环丁烷基序，在钙流量和 CTX 分析中的 IC₅₀ 为 22 nM 和 50 nM。CCR4 antagonist 3 具有抗肿瘤活性。

CCR4 antagonist 3 Chemical Structure

CAS No. : 2174938-70-4

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CCR4 antagonist 3 的其他形式现货产品:

CCR4 antagonist 3 hydrochloride

生物活性

CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC₅₀s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity^[1].

IC₅₀ & Target^[1]

CCR4

体外研究
(In Vitro)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor^[1]
Dosage:	50 mg/kg
Administration:	PO; daily; for 40 days
Result:	Significantly reduced the tumor growth.

Animal Model:	Rat and mouse^[1]
Dosage:	0.5 mg/kg of IV; 2 mg/kg of PO
Administration:	IV or PO
Result:	Possessed medium clearance (CL=47.6 mL/min/kg) and was 49% bioavailable upon oral dosing in rat. Had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

分子量

500.42

Formula

C₂₄H₂₇Cl₂N₇O

CAS 号

2174938-70-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Omar Robles, et al. Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as Single Agent and in Combination with Checkpoint Inhibitors. J Med Chem. 2020 Jul 15.

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ERRα antagonist-1

发表于2024年8月8日由上海金畔生物科技有限公司

ERRα antagonist-1 纯度: 98.48%

ERRα antagonist-1 (Compound A) 是一种选择性的，高亲和力的雌激素相关受体α (ERRα) 拮抗剂。ERRα antagonist-1 抑制 ERRα 与增殖物激活的受体γ共激活因子 1α (PGC-1α) 和 PGC-1β 的相互作用，IC₅₀ 值分别为 170 nM 和 180 nM。ERRα antagonist-1 不抑制 ERRβ 或 ERRγ 与 PGC-1α 和 PGC-1β 共激活剂的相互作用，也不抑制 ERα 或 ERβ 与 PGC-1α 或 SRC-1 的相互作用。

ERRα antagonist-1 Chemical Structure

CAS No. : 1072145-33-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥935	In-stock
5 mg	￥850	In-stock
10 mg	￥1500	In-stock
25 mg	￥3000	In-stock
50 mg	￥4500	In-stock
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ERRα antagonist-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library
Anti-Breast Cancer Compound Library

生物活性

ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC₅₀ values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1^[1].

IC₅₀ & Target^[1]

ERRα

分子量

377.53

Formula

C₂₁H₁₉N₃S₂

CAS 号

1072145-33-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 7.14 mg/mL (18.91 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6488 mL	13.2440 mL	26.4880 mL
5 mM	0.5298 mL	2.6488 mL	5.2976 mL
10 mM	0.2649 mL	1.3244 mL	2.6488 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 0.71 mg/mL (1.88 mM); Clear solution

此方案可获得 ≥ 0.71 mg/mL (1.88 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Michael J. Chisamore, et al. Identification of Small Molecule Estrogen-Related

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LPA2 antagonist 1

发表于2024年8月5日由上海金畔生物科技有限公司

LPA2 antagonist 1 纯度: 99.56%

LPA2 antagonist 1是LPA2的拮抗剂，IC₅₀值为17 nM。

LPA2 antagonist 1 Chemical Structure

CAS No. : 1017606-66-4

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10 mM * 1 mL in DMSO	￥3854	In-stock
2 mg	￥2333	In-stock
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg	￥15000	In-stock
100 mg	￥21000	In-stock
200 mg		询价
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LPA2 antagonist 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
GPCR/G Protein Compound Library
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Targeted Diversity Library

生物活性

LPA2 antagonist 1 is a LPA2 antagonist with an IC₅₀ of 17 nM.

IC₅₀ & Target

IC50: 17 nM (LPA2)^[1]

体外研究
(In Vitro)

LPA2 antagonist 1 inhibits the phosphorylation of Erk induced by LPA in a concentration dependent manner. LPA2 antagonist 1 inhibits HCT-116 colon cancer cell proliferation caused by LPA in a doses dependent manner^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

500.46

Formula

C₂₀H₂₃Cl₂N₅O₂S₂

CAS 号

1017606-66-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMF : ≥ 100 mg/mL (199.82 mM)

DMSO : ≥ 100 mg/mL (199.82 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9982 mL	9.9908 mL	19.9816 mL
5 mM	0.3996 mL	1.9982 mL	3.9963 mL
10 mM	0.1998 mL	0.9991 mL	1.9982 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.00 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Beck HP, et al. Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1037-41.

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Mcl-1 antagonist 1

发表于2024年7月30日由上海金畔生物科技有限公司

Mcl-1 antagonist 1

Mcl-1 antagonist 1 是一种 Mcl-1 拮抗剂，详细信息请参考专利文献 WO2019173181 中的化合物 200。

Mcl-1 antagonist 1 Chemical Structure

CAS No. : 2376775-05-0

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生物活性	Mcl-1 antagonist 1 is a Mcl-1 protein antagonist extracted from patent WO2019173181, compound 200^[1].
分子量	850.41
Formula	C₄₁H₅₄ClF₂N₅O₈S
CAS 号	2376775-05-0
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Gwenaella Rescourio, et al. Alpha-hydroxy phenylacetic acid pharmacophore or bioisostere mcl-1 protein antagonists. WO2019173181.

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EP4 receptor antagonist 2

发表于2024年7月28日由上海金畔生物科技有限公司

EP4 receptor antagonist 2

EP4 receptor antagonist 2 (compound 2-13) 是一种有效的 EP4 受体激动剂，IC₅₀ 值为 7.8 nM。EP4 receptor antagonist 2 具有抗肿瘤活性。

EP4 receptor antagonist 2 Chemical Structure

CAS No. : 1965316-82-8

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生物活性

EP4 receptor antagonist 2 (compound 2-13) is a potent EP4 receptor antagonist with an IC₅₀ of 7.8 nM. EP4 receptor antagonist 2 shows antitumor activity^[1].

IC₅₀ & Target^[1]

EP4

7.8 nM (IC₅₀)

分子量

475.54

Formula

C₂₇H₂₉N₃O₅

CAS 号

1965316-82-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. TRICYCLIC SPIRO COMPOUND.

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AHR antagonist 5

发表于2024年7月23日由上海金畔生物科技有限公司

AHR antagonist 5

AHR antagonist 5 是有效的，具有口服活性的芳香烃受体 (AHR) 拮抗剂，IC₅₀ 为 < 0.5 μM。AHR antagonist 5 联合检测点抑制剂 anti-PD-1 对肿瘤生长有抑制作用，详细信息请参见专利 WO2018195397，example 39。

AHR antagonist 5 Chemical Structure

CAS No. : 2247953-39-3

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5 mg	￥6600	询问价格 & 货期
10 mg	￥10500	询问价格 & 货期

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生物活性

AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC₅₀ of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1^[1].

体内研究
(In Vivo)

Tumor growth inhibition is statistically significant with AHR antagonist 5 as single. AHR antagonist 5 (10 mg/kg; p.o.; every day for 3 weeks) combination with anti-PD-1 significantly inhibited tumor growth inhibition compared to the anti-PD-1 alone^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Balb/c Mice (Mouse Colorectal Cancer Model CT26)^[1]
Dosage:	10 mg/kg (combination with anti-PD-1)
Administration:	P.o.; every day for 3 weeks
Result:	Significantly inhibited tumor growth inhibition.

分子量

550.89

Formula

C₂₅H₂₇Cl₃FN₇

CAS 号

2247953-39-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Alfredo C. Castro, et al. Indole ahr inhibitors and uses thereof. WO2018195397A2.

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CCR4 antagonist 2

发表于2024年6月29日由上海金畔生物科技有限公司

CCR4 antagonist 2

CCR4 antagonist 2 (Compound 31) 是一种新的有效，口服生物可利用的趋化因子受体 4 (CCR4) 的小分子拮抗剂，其抑制T_reg 贩运进入肿瘤微环境而不影响健康组织中 T_reg 的数量。 CCR4 antagonist 2 (Compound 31) 抑制 Ca²⁺ flux 和 CTX 的 IC₅₀ 值分别为 40 nM 和 70 nM。

CCR4 antagonist 2 Chemical Structure

CAS No. : 2206788-99-8

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生物活性	CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits T_reg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC₅₀ values of Ca²⁺flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively^[1].
IC₅₀ & Target	IC50: 40 nM (Ca²⁺flux); 70 nM (CTX) (CCR4 antagonist 2)^[1]
分子量	511.45
Formula	C₂₆H₂₈Cl₂N₆O
CAS 号	2206788-99-8
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Jackson JJ, et al. Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment. J Med Chem. 2019 Jul 11;62(13):6190-6213.

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EP4 receptor antagonist 1

发表于2024年5月25日由上海金畔生物科技有限公司

EP4 receptor antagonist 1

EP4 receptor antagonist 1 是一种高效的，竞争性的，选择性前列腺素类 EP4 受体拮抗剂。可用于癌症免疫研究。EP4 receptor antagonist 1 抑制人和小鼠 EP4 受体，IC₅₀ 分别为 6.1 nM 和 16.2 nM。对人 EP1，EP2 和 EP3 受体的 IC₅₀ >10 μM。

EP4 receptor antagonist 1 Chemical Structure

CAS No. : 2287259-07-6

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250 mg		询价
500 mg		询价

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生物活性

EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC₅₀s of 6.1 nM and 16.2 nM, respectively. IC₅₀s >10 μM for human EP1, EP2,and EP3 receptors^[1].

IC₅₀ & Target

IC50: 6.1 nM (human EP4 receptor), 16.2 nM (mouse EP4 receptor)^[1]

体外研究
(In Vitro)

The antagonistic effect of EP4 receptor antagonist 1 (Compounds 59) on human EP4 in calcium flux assay with an IC₅₀ of 6.1±0.2 nM in CHO-G_α16 cells overexpressing human EP4 receptor. The antagonistic effect of EP4 receptor antagonist 1 on human EP4 in calcium flux assay with an IC₅₀ of 16.2±1.7 nM in CHO-G_α16 cells overexpressing mouse EP4 receptor^[1].
EP4 receptor antagonist 1 dose dependently inhibits PGE2-stimulated cAMP accumulation in HEK293-EP4 cells with an IC₅₀ of 18.7±0.6 nM. EP4 receptor antagonist 1 dose-dependently inhibits the activity of the CRE reporter in HEK293 cells with an IC₅₀ of 5.2±0.4 nM.EP4 receptor antagonist 1 dose-dependently inhibits PGE2-stimulated β-arrestin recruitment in HEK293-EP4 cells with an IC₅₀ of 0.4±0.1 nM^[1].
EP4 receptor antagonist 1 (1 nM-10 μM) reverses PGE2-induced ERK phosphorylation in a concentration-dependent manner^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	CHO-EP4 cells
Concentration:	1 nM, 100 nM, 10 μM
Incubation Time:	Pretreated for 20 min and then subjected to 30 nM PGE2 simulation for 10 min.
Result:	Reversed PGE2-induced ERK phosphorylation in a concentration-dependent manner.

体内研究
(In Vivo)

EP4 receptor antagonist 1 (16, 50, and 150 mg/kg; orally; once daily for two weeks) causes significant inhibition of tumor growth in BALB/c female mice. No significant body weight loss is found in any mouse cohorts. EP4 receptor antagonist 1 is well tolerated in mice at the tested dosage^[1].
EP4 receptor antagonist 1 (1 mg/kg; intravenously) demonstrates moderate clearance (CL=1.7 L/h/kg) in mice with a corresponding favorable half-life (t_1/2) of 4.1 h. EP4 receptor antagonist 1 (5 mg/kg; orally) exhibits good bioavailability (F=48.0%) in mice with a corresponding favorable half-life (t_1/2) of 4.7 h^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c female mice (6-week-old)bearing CT26 colon cancer model^[1]
Dosage:	16, 50, and 150 mg/kg
Administration:	Orally; once daily for two weeks
Result:	Tumor growth inhibition (TGI) was 24.6% at 16 mg/ kg, 54.7% at 50 mg/kg, and 63.8% at 150 mg/kg.

Animal Model:	BALB/c female mice^[1]
Dosage:	1 mg/kg and 5 mg/kg (Pharmacokinetic Analysis)
Administration:	Intravenously or orally at a dose of 1 mg/kg (5 mL/kg) and 5 mg/kg (10 mL/kg),respectively.
Result:	Demonstrated moderate clearance ( CL=1.7 L/h/kg) in mice with a corresponding favorable half-life (t_1/2) of 4.1 h at a dose of 1 mg/kg (intravenously). Exhibited good bioavailability (F=48.0%) in mice with a corresponding favorable half-life (t_1/2) of 4.7 h at a dose of 5 mg/kg (orally).

分子量

458.43

Formula

C₂₃H₂₁F₃N₄O₃

CAS 号

2287259-07-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Yang JJ, et al. Discovery and Characterization of 1H-1,2,3-Triazole Derivatives as Novel Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2020 Jan 23;63(2):569-590.

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AHR antagonist 5 hemimaleate

发表于2024年5月17日由上海金畔生物科技有限公司

AHR antagonist 5 hemimaleate

AHR antagonist 5 hemimaleate 是有效的，具有口服活性的芳香烃受体 (AHR) 拮抗剂，IC₅₀ 为 < 0.5 μM。AHR antagonist 5 hemimaleate 联合检测点抑制剂 anti-PD-1 对肿瘤生长有抑制作用，详细信息请参见专利 WO2018195397，example 39。

AHR antagonist 5 hemimaleate Chemical Structure

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生物活性	AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC₅₀ of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39)^[1].
体外研究 (In Vitro)	Tumor growth inhibition is statistically significant with AHR antagonist 5 as single. AHR antagonist 5 (10 mg/kg; p.o.; every day for 3 weeks) combination with anti-PD-1 significantly inhibited tumor growth inhibition compared to the anti-PD-1 alone^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	499.55
Formula	C₂₉H₂₈FN₇O₄
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Alfredo C. Castro, et al. Indole ahr inhibitors and uses thereof. WO2018195397A2.

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多肽定制Antagonist G 编码

发表于2024年5月16日由上海金畔生物科技有限公司

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称	Antagonist G
编码
别名	Antagonist G
纯度	80%，90%，95%，98%，99%
重量	1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写）	R-DTrp-(Nme)Phe-DTrp-LM-NH2
序列（三字母缩写）	H-Arg-DTrp-(Nme)Phe-DTrp-Leu-Met-NH2?(trifluoroacetate salt)
基本描述
溶解度
分子量	951.2
化学式	C49H66N12O6S1
存储条件	Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
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Figures
Reference
C端
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化学桥

TMBIM6 antagonist-1

发表于2024年5月5日由上海金畔生物科技有限公司

TMBIM6 antagonist-1 纯度: 99.80%

TMBIM6 antagonist-1 是一个有潜力的 TMBIM6 拮抗剂，抑制 TMBIM6 与 mTORC2 结合，降低 mTORC2 活性，调节TMBIM6 释放 Ca²⁺。

TMBIM6 antagonist-1 Chemical Structure

CAS No. : 123134-61-2

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5 mg	￥2500	In-stock
10 mg	￥4000	In-stock
50 mg	￥11500	In-stock
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TMBIM6 antagonist-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca²⁺^[1].

体外研究
(In Vitro)

TMBIM6 antagonist-1 (BIA, 0.5-10 μM, 3 days) significantly and dose-dependently inhibits cell viability in HT1080, MCF7, MDA-MB-2341 and SKBR3 cells, with IC₅₀ values of 1.7 ± 0.1 μM for HT1080, 2.6 ± 0.4 μM for MCF cells, 2.6 ± 0.5 μM for MDA-MB-231 cells, and 2.4 ± 0.4 μM for SKBR3 cells, respectively^[1].
TMBIM6 antagonist-1 (BIA, 10 μM) treatment decreases cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells, not TMBIM6 KO HT1080 cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	HT1080, MCF7, MDA-MB-2341 and SKBR3 cells.
Concentration:	0.5-10 μM.
Incubation Time:	3 days.
Result:	Inhibited cell viability.

Western Blot Analysis^[1]

Cell Line:	WT and TMBIM6 KO HT1080 cells.
Concentration:	0, 2, 5 μM.
Incubation Time:
Result:	Downregulated the protein levels of AKT-pS473.

体内研究
(In Vivo)

TMBIM6 antagonist-1 (1 mg/kg, IP 5 days per week during 25 days) significantly impaires cell-driven tumor growth^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six- to eight-week BklNbt:BALB/c/nu/nu old mice (HT1080 and MDA-MB-231 cells)^[1].
Dosage:	1 mg/kg.
Administration:	IP 5 days per week during 25 days.
Result:	Impaired cell-driven tumor growth.

分子量

268.27

Formula

C₁₅H₁₂N₂O₃

CAS 号

123134-61-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (186.38 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7276 mL	18.6379 mL	37.2759 mL
5 mM	0.7455 mL	3.7276 mL	7.4552 mL
10 mM	0.3728 mL	1.8638 mL	3.7276 mL

参考文献

[1]. Hyun-Kyoung Kim, et al. TMBIM6/BI-1 contributes to cancer progression through assembly with mTORC2 and AKT activation. Nat Commun. 2020 Aug 11;11(1):4012.

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Adenosine receptor antagonist 2

发表于2024年4月29日由上海金畔生物科技有限公司

Adenosine receptor antagonist 2

Adenosine receptor antagonist 2 是一种口服有效的 A2a/A2b 腺苷受体拮抗剂，IC₅₀ 分别为 1 nM 和 3 nM。Adenosine receptor antagonist 2 具有抗肿瘤活性。

Adenosine receptor antagonist 2 Chemical Structure

CAS No. : 2703054-47-9

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生物活性

Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC₅₀s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity^[1].

IC₅₀ & Target^[1]

A2a adenosine receptor

1 nM (IC₅₀)

A2b adenosine receptor

3 nM (IC₅₀)

体内研究
(In Vivo)

Adenosine receptor antagonist 2 (compound L-1; po; 10, 30, 100 mg/kg; twice a day for 22 days) inhibits tumor growth in female C57BL / 6mice mice with MC38(#22)-hpd-L1 cells^[1].
Adenosine receptor antagonist 2 (iv; 2 mg/kg) has a CLz of 14.7 mL/min·kg and an AUC of 2252 h·ng/mL. Adenosine receptor antagonist 2 (po; 10 mg/kg) has a C_max of 8730 ng/mL in adult male ICR mice (weight 25-40g)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

444.46

Formula

C₂₃H₂₁FN₈O

CAS 号

2703054-47-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Lifeng Liu, et al. Substituted pyrimidine or Pyridylamine derivatives, their compositions and pharmaceutical uses. WO2021185256A1.

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Adenosine receptor antagonist 3

发表于2024年4月28日由上海金畔生物科技有限公司

Adenosine receptor antagonist 3

Adenosine receptor antagonist 3 是一种有效的腺苷受体拮抗剂。Adenosine receptor antagonist 3 具有研究癌症疾病的潜力 (摘自专利 WO2019233994A1，化合物1)。

Adenosine receptor antagonist 3 Chemical Structure

CAS No. : 2400864-80-2

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生物活性	Adenosine receptor antagonist 3 is a potent antagonist of adenosine receptor. Adenosine receptor antagonist 3 has the potential for the research of cancer disease (extracted from patent WO2019233994A1, compound 1)^[1].
分子量	322.39
Formula	C₁₆H₁₄N₆S
CAS 号	2400864-80-2
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Andrew Simon Bell, et al. Pyrazolopyrimidine compounds as adenosine receptor antagonists. Patent WO2019233994A1.

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Estrogen receptor antagonist 2

发表于2024年4月14日由上海金畔生物科技有限公司

Estrogen receptor antagonist 2

Estrogen receptor antagonist 2 是一种选择性的 estrogen receptor 下调剂。雌激素 (E2) 和雌激素 α 受体 (ERα) 是乳腺癌发展的重要驱动因素。Estrogen receptor antagonist 2 具有研究乳腺癌疾病的潜力 (摘自专利 WO2021228210A1，化合物 3)。

Estrogen receptor antagonist 2 Chemical Structure

CAS No. : 2735803-90-2

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生物活性	Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3)^[1].
分子量	489.55
Formula	C₂₆H₃₁F₄N₅
CAS 号	2735803-90-2
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Gu Peng, et al. Pyrrolidine compounds and their applications. Patent WO2021228210A1.

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whatman (沃特曼)

英国沃特曼 Millipore PALL中国代理商金畔官网

标签归档：antagonist

AHR antagonist 5 free base

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ERRα antagonist-1 相关产品

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LPA2 antagonist 1 相关产品

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Mcl-1 antagonist 1

EP4 receptor antagonist 2

AHR antagonist 5

CCR4 antagonist 2

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AHR antagonist 5 hemimaleate

多肽定制Antagonist G 编码

TMBIM6 antagonist-1

TMBIM6 antagonist-1 相关产品

•相关化合物库:

Adenosine receptor antagonist 2

Adenosine receptor antagonist 3

Estrogen receptor antagonist 2