Encequidar (HM30181)

An inhibitor of P-glycoprotein

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥1287.00

1030.00

- +
10mg

￥1937.00

1550.00

- +
50mg

￥5775.00

4620.00

- +
100mg

￥9150.00

7320.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

Background

HM30181 is an inhibitor of P-glycoprotein (P-gp), also known as multidrug resistance protein 1 (MDR1; IC₅₀ = 0.63 nM).¹ It is selective for P-gp over breast cancer resistance protein (BCRP; IC₅₀ = 3,700 nM), as well as multidrug resistance-associated protein 1 (MRP1), MRP2, and MRP3 at 100 ?M. It inhibits transepithelial basal-to-apical transport of paclitaxel in MDCK monolayers overexpressing P-gp (IC₅₀ = 35.4 nM). HM30181 inhibits tumor growth and induces tumor regression in an HT-29 mouse xenograft model when administered at doses of 10 and 20 mg/kg, respectively, in combination with paclitaxel .

1.Kwak, J.-O., Lee, S.H., Lee, G.S., et al.Selective inhibition of MDR1 (ABCB1) by HM30181 increases oral bioavailability and therapeutic efficacy of paclitaxelEur. J. Pharmacol.627(1-3)92-98(2009)

Protocol

Animal experiment:

Mice[1]Encequidar (HM30181) mesylate is dissolved in 5% aqueous glucose solution, containing 20 μL 0.01 M aq. HCl and injected at a volume of 4 mL/kg. Female FVB wild-type mice, aged 8-12 weeks weighing 24±4 g undergo (R)-[11C]verapamil PET scans without and with i.v. pretreatment with cold Encequidar (HM30181). Animals are assigned to 5 groups (n=4 per group). One group is pretreated with HM30181 vehicle solution (5% aq. glucose solution containing 20 μL 0.01 M aq. HCl) at 60 min before start of the PET scan. The other groups are pretreated with either 10 mg/kg Encequidar (HM30181) at 10, 60 or 120 min before PET or with 21 mg/kg HM30181 at 10 min before PET[1].

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.