EG01377 dihydrochloride|西域试剂

EG01377 dihydrochloride,99.19%

产品编号：Bellancom-112151A| 分子式：C₂₆H₃₂Cl₂N₆O₆S₂| 分子量：659.60

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-112151A	￥4500.00	杭州北京（现货）
Bellancom-112151A	￥7500.00	杭州北京（现货）
Bellancom-112151A	￥21000.00	杭州北京（现货）
Bellancom-112151A	￥33500.00	杭州北京（现货）

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EG01377 dihydrochloride

产品介绍

EG01377 dihydrochloride 是有效的、可生物利用的和选择性的 neuropilin-1 (NRP1) 抑制剂，K_d 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。

生物活性

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

体外研究

EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR.
EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA.
EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure.
EG01377 (30 μM) reduces network area, length, and branching points.
EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis.
EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 week-old BABL/c female mice
Dosage:	2 mg/kg (Pharmacokinetic Analysis)
Administration:	I.v. administration
Result:	The half time (T_1/2) of 4.29 h.

体内研究

EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 week-old BABL/c female mice
Dosage:	2 mg/kg (Pharmacokinetic Analysis)
Administration:	I.v. administration
Result:	The half time (T_1/2) of 4.29 h.

体内研究

EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 week-old BABL/c female mice
Dosage:	2 mg/kg (Pharmacokinetic Analysis)
Administration:	I.v. administration
Result:	The half time (T_1/2) of 4.29 h.

性状

Solid

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。