HM-30181-A

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Encequidar；HM30181；HM30181A

DMSO : 2.4 mg/mL (3.48 mM; Need ultrasonic)

P-glycoprotein

HM30181 is shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC_50, tariquidar: 8.2±2.0 nM, HM30181: 13.1±2.3 nM) . 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.

PET scans with the Pgp substrate (R)-verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failes to show significant increases in (R)-verapamil brain uptake compared with vehicle treated animals. 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. HM30181 increases the oral bioavailability of co-administered paclitaxel by more than 12 times in rats.