标签归档：nrp

EG01377 dihydrochloride

发表于由

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。

EG01377 dihydrochloride  纯度: 98.21%

EG01377 dihydrochloride 是有效的、可生物利用的和选择性的 neuropilin-1 (NRP1) 抑制剂，Kd 值为 1.32 μM，对 NRP1-a1 和 NRP1-b1 的 IC50 值均为 609 nM。EG01377 dihydrochloride 具有抗血管生成，抗迁移及抗肿瘤等活性。

EG01377 dihydrochloride

EG01377 dihydrochloride Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥6530 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg ￥21000 In-stock
100 mg ￥33500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

EG01377 dihydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library

生物活性

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects[1].

IC50 & Target

IC50: 609 nM (NRP1-a1 and NRP1-b)[1]
体外研究
(In Vitro)

EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR[1].
EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA[1].
EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure[1].
EG01377 (30 μM) reduces network area, length, and branching points[1].
EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis[1].
EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth[1].
EG01377 (500 nM; 2 hours) blocks the production of transforming growth factor beta (TGFβ) by Nrp1+ regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors[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.

Western Blot Analysis[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 3, 10, 30 μM
Incubation Time: 30 minutes
Result: Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM.

体内研究
(In Vivo)

EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice[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: 6-8 week-old BABL/c female mice[1]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: I.v. administration
Result: The half time (T1/2) of 4.29 h.

分子量

659.60

Formula

C26H32Cl2N6O6S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
溶解性数据
In Vitro: 

DMSO : 200 mg/mL (303.21 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5161 mL 7.5804 mL 15.1607 mL
5 mM 0.3032 mL 1.5161 mL 3.0321 mL
10 mM 0.1516 mL 0.7580 mL 1.5161 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 (stored under nitrogen, away from moisture)。-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：

——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: ≥ 5 mg/mL (7.58 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (7.58 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (7.58 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (7.58 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (7.58 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (7.58 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 50.0 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]. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135-4154.

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

EG00229

发表于由

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。

EG00229  纯度: 98.89%

EG00229 是一种神经纤维蛋白 1 受体 (NRP1) 拮抗剂。EG00229 选择性抑制 VEGF-A 与 NRP1 b1 域的结合， IC50 为 3μM，但对 VEGFA 与 VEGFR-1 和 VEGFR-2 的结合没有影响。

EG00229

EG00229 Chemical Structure

CAS No. : 1210945-69-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1884 In-stock
5 mg ￥1400 In-stock
10 mg ￥2250 In-stock
50 mg ￥8980 In-stock
100 mg ￥15400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

EG00229 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Peptidomimetic Library

生物活性

EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2[1].

IC50 & Target

IC50: 8 μM (125I-VEGF-A binding to PAE/NRP1); 3 μM (bt-VEGF-A binding to purified NRP1 b1 domain)[1].
体外研究
(In Vitro)

EG00229 (Compound 2; 0-100 μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation[1].
EG00229 (Compound 2) demonstrates inhibition of VEGF-A binding to NRP1 and attenuates VEGFR2 phosphorylation in endothelial cells. Inhibition of migration of endothelial cells is also observed in HUVECs[1].
EG00229 (Compound 2) selectively inhibits radiolabeled 125I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1, but not VEGFR2-expressing cells, with an IC50 of 8 μM. EG00229 also inhibits VEGF-A binding to lung carcinoma A549 and prostate carcinoma DU145 cells, which express NRP1, but not VEGFR1 and VEGFR2, with similar potency. Binding of VEGF-A to human umbilical vein endothelial cells (HUVECs), which express VEGFR2, VEGFR1, and NRP1, is also inhibited by EG00229 with an IC50 of 23 μM[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: A549 cells
Concentration: 0 µM, 10 μM, 30 μM, 100 μM
Incubation Time: 48 hours
Result: Caused a significant reduction in cell viability.

体内研究
(In Vivo)

EG00229 (0-10 mg/kg; intraperitoneal injection; three times per week; for 4 weeks; NSG mice) treatment substantially reduces tumor growth and visible vascularization[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.

Animal Model: 6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells[2]
Dosage: 0 mg/kg, 10 mg/kg
Administration: Intraperitoneal injection; three times per week; for 4 weeks
Result: Reduces tumor growth and visible vascularization.

分子量

611.60

Formula

C19H20F3N7O7S3
CAS 号

1210945-69-9
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 : ≥ 41.4 mg/mL (67.69 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 1.6351 mL 8.1753 mL 16.3506 mL
5 mM 0.3270 mL 1.6351 mL 3.2701 mL
10 mM 0.1635 mL 0.8175 mL 1.6351 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 (sealed storage, away from moisture)。-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：

——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: ≥ 2.5 mg/mL (4.09 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.09 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 (4.09 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.09 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]. Jarvis A, et al. Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. J Med Chem. 2010 Mar 11;53(5):2215-26.

    [2]. Grun D, et al. VEGF-A acts via neuropilin-1 to enhance epidermal cancer stem cell survival and formation of aggressive and highly vascularized tumors. Oncogene. 2016 Aug 18;35(33):4379-87.

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

EG01377

发表于由

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。

EG01377 

EG01377 是有效的、可生物利用的和选择性的 neuropilin-1 (NRP1) 抑制剂，Kd 值为 1.32 μM，对 NRP1-a1 和 NRP1-b1 的 IC50 值均为 609 nM。EG01377 具有抗血管生成，抗迁移及抗肿瘤等活性。

EG01377

EG01377 Chemical Structure

CAS No. : 2227996-00-9

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

* Please select Quantity before adding items.

EG01377 的其他形式现货产品:

EG01377 dihydrochloride

生物活性

EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects[1].

IC50 & Target

IC50: 609 nM (NRP1-a1 and NRP1-b)[1] Kd: 1.32 μM (NRP1-b1)[1]
体外研究
(In Vitro)

EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR[1].
EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA[1].
EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure[1].
EG01377 (30 μM) reduces network area, length, and branching points[1].
EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis[1].
EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth[1].
EG01377 (500 nM; 2 hours) blocks the production of transforming growth factor beta (TGFβ) by Nrp1+ regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors[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.

Western Blot Analysis[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 3, 10, 30 μM
Incubation Time: 30 minutes
Result: Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM.

体内研究
(In Vivo)

EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice[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: 6–8 week-old BABL/c female mice[1]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: I.v. administration
Result: The half time (T1/2) of 4.29 h.

分子量

586.68

Formula

C26H30N6O6S2
CAS 号

2227996-00-9
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]. Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135-4154.

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

NRP1 antagonist 2

发表于由

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。

NRP1 antagonist 2 

NRP1 antagonist 2 (Compound 1) 是一种 NRP1 拮抗剂。

NRP1 antagonist 2

NRP1 antagonist 2 Chemical Structure

CAS No. : 483289-96-9

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

NRP1 antagonist 2 (Compound 1) is an NRP1 antagonist[1].

IC50 & Target

NRP1[1]
分子量

456.97

Formula

C20H17ClN6OS2
CAS 号

483289-96-9
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]. Peng K, et al. Discovery of novel nonpeptide small-molecule NRP1 antagonists: Virtual screening, molecular simulation and structural modification. Bioorg Med Chem. 2020 Jan 1;28(1):115183.

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