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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-P-glycoprotein (P-gp)-Encequidar
Encequidar

Chemical Structure : Encequidar

CAS No.: 849675-66-7

Encequidar (HM30181, HM30181A)

货号: PC-73218Not For Human Use, Lab Use Only.

Encequidar (HM30181) is a potent selective inhibitor of MDR1 (ABCB1, P-gp) with IC50 of 0.63 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Encequidar (HM30181) is a potent selective inhibitor of MDR1 (ABCB1, P-gp) with IC50 of 0.63 nM.
Encequidar (HM30181) effectively blocked transepithelial transport of paclitaxel in MDCK monolayers.
Encequidar (HM30181) does not inhibit MRP1 (ABCC1), MRP2 (ABCC2), and MRP3 (ABCC3), and partially inhibited BCRP (ABCG2) only at very high concentrations.
Oral co-administration of paclitaxel and HM30181 showed a tumor-inhibitory strength equal or superior to that of intravenous paclitaxel in the xenograft model in nude mice.

物理化学性质&存储条件

分子量 688.741
分子式 C38H36N6O7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-(2-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl)-4-oxo-4H-chromene-2-carboxamide

参考文献

1. Kim TE, et al. Br J Clin Pharmacol. 2014 Sep;78(3):556-64.

2. Bauer F, et al. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27.

3. Kwak JO, et al. Eur J Pharmacol. 2010 Feb 10;627(1-3):92-8.

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