CXCR4 antagonist 5

发表于2024年12月22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。

CXCR4 antagonist 5

CXCR4 antagonist 5 (compound 23) 是一种高效的 CXCR4 拮抗剂，IC₅₀ 为 8.8 nM。CXCR4 antagonist 5 可抑制 CXCL12 诱导的胞质钙离子增加 (IC₅₀ = 0.02 nM)，也能抑制 CXCR4/CXLC12 介导的趋化作用。CXCR4 antagonist 5 具有良好的理化性质和体外安全性，轻度或中度抑制 CYP 同工酶和 hERG。

CXCR4 antagonist 5 Chemical Structure

CAS No. : 2304749-86-6

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生物活性

CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC₅₀ value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC₅₀ = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately^[1].

IC₅₀ & Target^[1]

CXCR4

8.8 nM (IC₅₀)

分子量

366.50

Formula

C₂₁H₃₀N₆

CAS 号

2304749-86-6

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]. Zhu F, et al. Structural optimization of aminopyrimidine-based CXCR4 antagonists. Eur J Med Chem. 2020;187:111914.

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CXCR4 antagonist 6

发表于2024年12月21日由上海金畔生物科技有限公司

CXCR4 antagonist 6

CXCR4 antagonist 6 (compound 46) 是一种有效的 CXCR4 拮抗剂，IC₅₀ 为 79 nM。CXCR4 antagonist 6 可抑制 CXCL12 诱导的胞质钙离子流量 (IC₅₀ = 0.25 nM)。CXCR4 antagonist 6 显著减弱 CXCL12/CXCR4 介导的细胞迁移。CXCR4 antagonist 6 在小鼠肿瘤转移模型中显示出显著的抗肿瘤效果。

CXCR4 antagonist 6 Chemical Structure

CAS No. : 2304750-68-1

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生物活性

CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC₅₀ value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC₅₀ = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice^[1].

IC₅₀ & Target^[1]

CXCR4

79 nM (IC₅₀)

分子量

366.50

Formula

C₂₁H₃₀N₆

CAS 号

2304750-68-1

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]. Li Z, et al. Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity. Eur J Med Chem. 2020;205:112537.

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CXCR2 antagonist 2

发表于2024年12月15日由上海金畔生物科技有限公司

CXCR2 antagonist 2

CXCR2 antagonist 2 是一种有效的癌症免疫治疗的 CXCR2 拮抗剂，IC₅₀ 值为 95 nM。

CXCR2 antagonist 2 Chemical Structure

CAS No. : 2647464-91-1

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生物活性	CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC₅₀ value of 95 nM.
分子量	364.39
Formula	C₁₇H₁₇FN₂O₄S
CAS 号	2647464-91-1
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]. Dong Y, et al. Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J Med Chem. 2021 Nov 25;64(22):16626-16640.

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CXCR2 antagonist 2

发表于2024年12月15日由上海金畔生物科技有限公司

CXCR2 antagonist 2

CXCR2 antagonist 2 是一种有效的癌症免疫治疗的 CXCR2 拮抗剂，IC₅₀ 值为 95 nM。

CXCR2 antagonist 2 Chemical Structure

CAS No. : 2647464-91-1

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生物活性	CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC₅₀ value of 95 nM.
分子量	364.39
Formula	C₁₇H₁₇FN₂O₄S
CAS 号	2647464-91-1
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]. Dong Y, et al. Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J Med Chem. 2021 Nov 25;64(22):16626-16640.

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CXCR2 antagonist 2

发表于2024年12月14日由上海金畔生物科技有限公司

CXCR2 antagonist 2

CXCR2 antagonist 2 是一种有效的癌症免疫治疗的 CXCR2 拮抗剂，IC₅₀ 值为 95 nM。

CXCR2 antagonist 2 Chemical Structure

CAS No. : 2647464-91-1

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生物活性	CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC₅₀ value of 95 nM.
分子量	364.39
Formula	C₁₇H₁₇FN₂O₄S
CAS 号	2647464-91-1
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]. Dong Y, et al. Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J Med Chem. 2021 Nov 25;64(22):16626-16640.

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CXCR2 antagonist 3

发表于2024年12月6日由上海金畔生物科技有限公司

CXCR2 antagonist 3

CXCR2 antagonist 3 (compound 11h) 是 CXC 趋化因子受体 2 (CXCR2) 的有效拮抗剂。CXCR2 antagonist 3 对 CXCR2 表现出两位数的纳摩尔效力，并显着抑制中性粒细胞浸润到气囊中。CXCR2 antagonist 3 可减少中性粒细胞和 MDSC 的浸润，并增强 CD3⁺ T 淋巴细胞向 Pan02 肿瘤组织的浸润。

CXCR2 antagonist 3 Chemical Structure

CAS No. : 2647464-92-2

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生物活性	CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3⁺ T lymphocytes into the Pan02 tumor tissues^[1].
分子量	362.38
Formula	C₁₇H₁₅FN₂O₄S
CAS 号	2647464-92-2
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]. Dong Y, et al. Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J Med Chem. 2021;64(22):16626-16640.

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CXCR2 antagonist 3

发表于2024年12月5日由上海金畔生物科技有限公司

CXCR2 antagonist 3

CXCR2 antagonist 3 Chemical Structure

CAS No. : 2647464-92-2

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生物活性	CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3⁺ T lymphocytes into the Pan02 tumor tissues^[1].
分子量	362.38
Formula	C₁₇H₁₅FN₂O₄S
CAS 号	2647464-92-2
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]. Dong Y, et al. Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J Med Chem. 2021;64(22):16626-16640.

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CXCR2 antagonist 3

发表于2024年12月5日由上海金畔生物科技有限公司

CXCR2 antagonist 3

CXCR2 antagonist 3 Chemical Structure

CAS No. : 2647464-92-2

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生物活性	CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3⁺ T lymphocytes into the Pan02 tumor tissues^[1].
分子量	362.38
Formula	C₁₇H₁₅FN₂O₄S
CAS 号	2647464-92-2
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]. Dong Y, et al. Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J Med Chem. 2021;64(22):16626-16640.

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NLRP3 antagonist 1

发表于2024年12月2日由上海金畔生物科技有限公司

NLRP3 antagonist 1

NLRP3 antagonist 1 是一种有效的 NLRP3 拮抗剂。NLRP3 主要在巨噬细胞和中性粒细胞中表达，参与机体对病原体感染和应激损伤的内在免疫。NLRP3 antagonist 1 具有研究癌症疾病的潜力 (信息摘自专利 WO2021114691A1，化合物3)。

NLRP3 antagonist 1 Chemical Structure

CAS No. : 2454017-83-3

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生物活性	NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body’s intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3)^[1].
分子量	310.35
Formula	C₁₆H₁₈N₆O
CAS 号	2454017-83-3
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]. Zejin You, et al. Nitrogen-containing and cyclic compounds, their preparation methods and uses. Patent WO2021114691A1.

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NLRP3 antagonist 1

发表于2024年12月2日由上海金畔生物科技有限公司

NLRP3 antagonist 1

NLRP3 antagonist 1 Chemical Structure

CAS No. : 2454017-83-3

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生物活性	NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body’s intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3)^[1].
分子量	310.35
Formula	C₁₆H₁₈N₆O
CAS 号	2454017-83-3
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]. Zejin You, et al. Nitrogen-containing and cyclic compounds, their preparation methods and uses. Patent WO2021114691A1.

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NLRP3 antagonist 1

发表于2024年12月2日由上海金畔生物科技有限公司

NLRP3 antagonist 1

NLRP3 antagonist 1 Chemical Structure

CAS No. : 2454017-83-3

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生物活性	NLRP3 antagonist 1 is a potent antagonist of NLRP3. NLRP3 is mainly expressed in macrophages and neutrophils and is involved in the body’s intrinsic immunity against pathogenic infections and stress injury. NLRP3 antagonist 1 has the potential for the research of cancer disease (extracted from patent WO2021114691A1, compound 3)^[1].
分子量	310.35
Formula	C₁₆H₁₈N₆O
CAS 号	2454017-83-3
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]. Zejin You, et al. Nitrogen-containing and cyclic compounds, their preparation methods and uses. Patent WO2021114691A1.

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TLR7/8 antagonist 1

发表于2024年11月26日由上海金畔生物科技有限公司

TLR7/8 antagonist 1

TLR7/8 Antagonist 1 (Compound 16c) 是 TLR7/8 的有效拮抗剂，IC₅₀ 值分别为 3.91 和 2.19 μM。TLR7/8 Antagonist 1 是一种咪唑喹啉衍生物化合物。Toll 样受体 (TLR) 7 和 8 是开发用于治疗传染病、癌症和自身免疫性疾病的免疫调节药物的关键靶点。

TLR7/8 antagonist 1 Chemical Structure

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生物活性	TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC₅₀s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders^[1].
分子量	417.50
Formula	C₂₄H₂₇N₅O₂
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 M, et al. Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs. Bioorg Med Chem Lett. 2022;59:128548.

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TLR7/8 antagonist 1

发表于2024年11月26日由上海金畔生物科技有限公司

TLR7/8 antagonist 1

TLR7/8 antagonist 1 Chemical Structure

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生物活性	TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC₅₀s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders^[1].
分子量	417.50
Formula	C₂₄H₂₇N₅O₂
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 M, et al. Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs. Bioorg Med Chem Lett. 2022;59:128548.

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TLR7/8 antagonist 1

发表于2024年11月26日由上海金畔生物科技有限公司

TLR7/8 antagonist 1

TLR7/8 antagonist 1 Chemical Structure

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生物活性	TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC₅₀s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders^[1].
分子量	417.50
Formula	C₂₄H₂₇N₅O₂
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 M, et al. Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs. Bioorg Med Chem Lett. 2022;59:128548.

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GRPR antagonist-1

发表于2024年11月25日由上海金畔生物科技有限公司

GRPR antagonist-1

GRPR antagonist-1 是一种有效的胃泌素释放肽受体 (GRPR) 拮抗剂，对某些癌细胞具有细胞毒性 (在PC3、Pan02、HGC-27 细胞中的 IC₅₀ 分别是 4.97、4.36、3.40 μM)。GRPR antagonist-1 通过降低 Bcl-2 水平、增加 Bax 水平，来抑制 HGC-27 细胞活力，引起细胞凋亡。具有抗癌活性。

GRPR antagonist-1 Chemical Structure

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生物活性

GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC₅₀ of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity^[1].

IC₅₀ & Target

IC₅₀: 4.97 μM (GRPR) in PC3, 4.36 μM (GRPR) in Pan02, 3.40 μM (GRPR) in HGC-27^[1]

体外研究
(In Vitro)

GRPR antagonist-1 (compound 5a) (0.032-100 μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM)^[1].
GRPR antagonist-1 (1, 2, 8 μM; 24 hours) increases the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells^[1].
GRPR antagonist-1 (0.8, 4 μM; 24 hours) inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis^[1].

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

Cell Proliferation Assay

Cell Line:	PC3, HepG2, HGC-27, Pan02, and HK2 cells^[1]
Concentration:	0.032-100 μM
Incubation Time:	48 hours
Result:	Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

Apoptosis Analysis

Cell Line:	HGC-27^[1]
Concentration:	1, 2, 8 μM
Incubation Time:	24 hours
Result:	Increased the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells.

Western Blot Analysis

Cell Line:	HGC-27^[1]
Concentration:	0.8, 4 μM
Incubation Time:	24 hours
Result:	Inhibited HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis.

分子量

558.59

Formula

C₂₉H₃₃F₃N₄O₄

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]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

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GRPR antagonist-2

发表于2024年11月25日由上海金畔生物科技有限公司

GRPR antagonist-2

GRPR antagonist-2 是一种有效的胃泌素释放肽受体 (GRPR) 拮抗剂，对某些癌细胞具有细胞毒性 (在 HGC-27 和 Pan02 细胞中的 IC₅₀ 分别是 0.77 和 2.5 μM)。具有抗癌活性。

GRPR antagonist-2 Chemical Structure

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生物活性

GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC₅₀ of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity^[1].

IC₅₀ & Target

IC₅₀: 0.77 μM (GRPR) in HGC-27, 2.5 μM (GRPR) in Pan02^[1]

体外研究
(In Vitro)

GRPR antagonist-2 (compound 6e) (0.032-100 μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM)^[1].

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

Cell Proliferation Assay

Cell Line:	PC3, HepG2, HGC-27, Pan02, and HK2 cells^[1]
Concentration:	0.032-100 μM
Incubation Time:	48 hours
Result:	Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

分子量

559.58

Formula

C₂₈H₃₂F₃N₅O₄

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]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

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AR antagonist 3

发表于2024年11月25日由上海金畔生物科技有限公司

AR antagonist 3

AR antagonist 3 是一种有效的选择性 androgen receptor (AR) 拮抗剂，IC₅₀ 为 0.47 µM。AR antagonist 3 呈剂量依赖性降低 FRET 信号 (IC₅₀= 18.05 μM)。当瘤内给药时，AR antagonist 3 可有效抑制肿瘤生长。

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

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生物活性

AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC₅₀ of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC₅₀= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally^[1].

IC₅₀ & Target

IC₅₀: 0.47 µM (AR)^[1]

体外研究
(In Vitro)

AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 µM) shows excellent AR antagonistic activity (eGFP IC₅₀= 0.47 μM; PSA IC₅₀= 1.42 μM)^[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) inhibits the proliferation of LNCaP cells^[1].
AR antagonist 3 (0.1, 1, 10 µM; 48 h) reduces the protein expression levels of c-Myc and KLK3^[1].
AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) exhibits a dose-dependent decrease of the FRET signal (IC₅₀= 18.05 μM)^[1].
AR antagonist 3 (10 µM; 2 h) reduces the DHT-mediated translocation of the AR into the nucleus in LNCaP cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	LNCaP-ARR2PB-eGFP cells
Concentration:	0.01, 0.1, 1, 10, 100 µM
Incubation Time:
Result:	Showed excellent AR antagonistic activity (eGFP IC₅₀= 0.47 μM; PSA IC₅₀= 1.42 μM).

Cell Proliferation Assay^[1]

Cell Line:	LNCaP, 22Rv1, C4-2, PC3, DU145 cells
Concentration:	0.01, 0.1, 1, 10, 100 µM
Incubation Time:	3 days
Result:	Inhibited the proliferation of LNCaP cells.

体内研究
(In Vivo)

AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65%^[1].

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

Animal Model:	6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g^[1]
Dosage:	2.5 mg/kg
Administration:	intratumorally injected; week; 25 days
Result:	Inhibited tumor growth and the final tumor growth inhibition is 65%.

分子量

306.38

Formula

C₁₅H₁₈N₂O₃S

CAS 号

349573-58-6

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]. Chai X, et al. Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2. J Med Chem. 2022, 65(3):2507-2521.

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GRPR antagonist-1

发表于2024年11月25日由上海金畔生物科技有限公司

GRPR antagonist-1

GRPR antagonist-1 Chemical Structure

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性

IC₅₀ & Target

IC₅₀: 4.97 μM (GRPR) in PC3, 4.36 μM (GRPR) in Pan02, 3.40 μM (GRPR) in HGC-27^[1]

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.

Cell Proliferation Assay

Cell Line:	PC3, HepG2, HGC-27, Pan02, and HK2 cells^[1]
Concentration:	0.032-100 μM
Incubation Time:	48 hours
Result:	Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

Apoptosis Analysis

Cell Line:	HGC-27^[1]
Concentration:	1, 2, 8 μM
Incubation Time:	24 hours
Result:	Increased the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells.

Western Blot Analysis

Cell Line:	HGC-27^[1]
Concentration:	0.8, 4 μM
Incubation Time:	24 hours
Result:	Inhibited HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis.

分子量

558.59

Formula

C₂₉H₃₃F₃N₄O₄

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]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GRPR antagonist-2

发表于2024年11月25日由上海金畔生物科技有限公司

GRPR antagonist-2

GRPR antagonist-2 Chemical Structure

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性

IC₅₀ & Target

IC₅₀: 0.77 μM (GRPR) in HGC-27, 2.5 μM (GRPR) in Pan02^[1]

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.

Cell Proliferation Assay

Cell Line:	PC3, HepG2, HGC-27, Pan02, and HK2 cells^[1]
Concentration:	0.032-100 μM
Incubation Time:	48 hours
Result:	Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

分子量

559.58

Formula

C₂₈H₃₂F₃N₅O₄

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]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AR antagonist 3

发表于2024年11月25日由上海金畔生物科技有限公司

AR antagonist 3

AR antagonist 3 Chemical Structure

CAS No. : 349573-58-6

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

IC₅₀ & Target

IC₅₀: 0.47 µM (AR)^[1]

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.

Cell Viability Assay^[1]

Cell Line:	LNCaP-ARR2PB-eGFP cells
Concentration:	0.01, 0.1, 1, 10, 100 µM
Incubation Time:
Result:	Showed excellent AR antagonistic activity (eGFP IC₅₀= 0.47 μM; PSA IC₅₀= 1.42 μM).

Cell Proliferation Assay^[1]

Cell Line:	LNCaP, 22Rv1, C4-2, PC3, DU145 cells
Concentration:	0.01, 0.1, 1, 10, 100 µM
Incubation Time:	3 days
Result:	Inhibited the proliferation of LNCaP cells.

体内研究
(In Vivo)

AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65%^[1].

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

Animal Model:	6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g^[1]
Dosage:	2.5 mg/kg
Administration:	intratumorally injected; week; 25 days
Result:	Inhibited tumor growth and the final tumor growth inhibition is 65%.

分子量

306.38

Formula

C₁₅H₁₈N₂O₃S

CAS 号

349573-58-6

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]. Chai X, et al. Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2. J Med Chem. 2022, 65(3):2507-2521.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

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

CXCR4 antagonist 5

CXCR4 antagonist 6

CXCR2 antagonist 2

CXCR2 antagonist 2

CXCR2 antagonist 2

CXCR2 antagonist 3

CXCR2 antagonist 3

CXCR2 antagonist 3

NLRP3 antagonist 1

NLRP3 antagonist 1

NLRP3 antagonist 1

TLR7/8 antagonist 1

TLR7/8 antagonist 1

TLR7/8 antagonist 1

GRPR antagonist-1

GRPR antagonist-2

AR antagonist 3

GRPR antagonist-1

GRPR antagonist-2

AR antagonist 3