HM30181 Formula: C38H36N6O7
HM30181 Solubility: DMSO: ≤ 6.6 mg/mL
HM30181 Purity: >98%
Please store the product under the recommended conditions in the Certificate of Analysis.
HM30181 is a potent and selective inhibitor of P-glycoprotein.
InVitro: 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, 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.
InVivo: PET scans with the Pgp substrate (R)-[ 11C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) failes to show significant increases in (R)-[ 11C]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.