Encequidar

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Chemical Structure| 849675-66-7 同义名 : HM30181; HM30181A
CAS号 : 849675-66-7
货号 : A658719
分子式 : C38H36N6O7
纯度 : 95+%
分子量 : 688.73
MDL号 : MFCD25976625
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(2.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 Encequidar demonstrates comparable potency to the reference Pgp inhibitor tariquidar in blocking rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, Encequidar: 13.1±2.3 nM) [1]. Encequidar (HM30181) exhibits high selectivity for mP-gp, with a potency 20-50 times greater than that of tariquidar, another third-generation P-gp inhibitor[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.45mL

0.29mL

0.15mL

7.26mL

1.45mL

0.73mL

14.52mL

2.90mL

1.45mL
参考文献

[1]Bauer F, et al. Interaction of HM30181 with P-glycoprotein at the murine blood-brain barrier assessed with positron emission tomography. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27.

[2]Kim TE, et al. Effects of HM30181, a P-glycoprotein inhibitor, on the pharmacokinetics and pharmacodynamics of loperamide in healthy volunteers. Br J Clin Pharmacol. 2014 Sep;78(3):556-64.