533794 Sigma-AldrichMDR1 Inhibitor, HM30181 - CAS 849675-66-7 - Calbiochem

This product has been discontinued.

A cell-permeable chromene-2-carboxamide compound that acts as a selective and highly potent inhibitor of the ATPase activity of multi-drug resistance protein 1 (MDR1, ABAC1, IC₅₀ = 630 pM). Does not affect MRP1, MRP2, MRP3, and has only a weak effect on BCRP (ABCG2) at higher concentrations. Shown to block trans-epithelial transport of paclitaxel in Madin-Darby canine kidney cells (MDCK; IC₅₀ = 35.5 nM). When co-administered (at 10 mg/kg, p.o.), it enhances the oral bioavailability of paclitaxel by about 12-fold and suppresses the growth of HT-29 tumor xenografts in nude mice (with 20 mg/kg paclitaxel, p.o.). Also shown to improve pharmacokinetic profile of paclitaxel (C_max = 1253 vs 127 ng/ml) without altering its half-life.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.