HM30181(Encequidar)|CAS 849675-66-7|DC Chemicals

Cas No.:	849675-66-7
Chemical Name:	Encequidar free base
Synonyms:	HM30181A
SMILES:	O=C(C1=CC(C2=CC=CC=C2O1)=O)NC3=CC(OC)=C(OC)C=C3C4=NN(C5=CC=C(CCN6CC7=C(C=C(OC)C(OC)=C7)CC6)C=C5)N=N4
Formula:	C₃₈H₃₆N₆O₇
M.Wt:	688.741
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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.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.

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