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Encequidar

CAS No. : 849675-66-7

MCE 站：Encequidar

产品活性：Encequidar (HM30181; HM30181A) 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; HM30181A) 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]NSC 657799 in FVB wild-type mice pretreated i.v. with Encequidar (HM30181) (10 or 21 mg/kg) failes to show significant increases in (R)-[¹¹C]NSC 657799 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 NSC 125973 by more than 12 times in rats.

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