HM30181;HM30181A Encequidar
- 公司名称 MedChemExpress LLC
- 品牌 MedChemExpress (MCE)
- 型号 HM30181;HM30181A
- 产地
- 厂商性质 生产厂家
- 更新时间 2019/7/11 13:47:45
- 访问次数 736
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供货周期 | 现货 | 规格 | 10 mM * 1 mL;5 mg;10 mg |
---|---|---|---|
货号 | HY-13646 | 应用领域 | 生物产业 |
Encequidar
产品活性:Encequidar (HM30181) 是一种有效的选择性的P-glycoprotein抑制剂。
研究领域:Membrane Transporter/Ion Channel
作用靶点:P-glycoprotein
In Vitro: Encequidar (HM30181) is shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, Encequidar (HM30181): 13.1±2.3 nM) . Encequidar (HM30181) shows a high selectivity for mP-gp and its potency is 20-50 times higher than that of tariquitar, another third generation P-gp inhibitor.
In Vivo: PET scans with the Pgp substrate (R)-[11C]verapamil in FVB wild-type mice pretreated i.v. with Encequidar (HM30181) (10 or 21 mg/kg) failes to show significant increases in (R)-[11C]verapamil brain uptake compared with vehicle treated animals. Encequidar (HM30181) inhibits P-gp mainly in the intestinal endothelium, which can be beneficial because pan-inhibition of P-gp, particularly in the brain, could lead to detrimental adverse events. Encequidar (HM30181) increases the oral bioavailability of co-administered paclitaxel by more than 12 times in rats.
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