Encequidar

849675-66-7

C38H36N6O7

DMSO : 6.9 mg/mL (10.02 mM; Need ultrasonic)

Membrane Transporter/Ion Channel

Encequidar (HM30181) is a potent and selective inhibitor of 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) ^[1]. 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^[2]. 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^[1]. 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^[2].