| Identification | Back Directory | [Name]
HM30181 (hydrochloride) | [CAS]
849675-88-3 | [Synonyms]
Encequidar, HCl
HM30181 (hydrochloride)
N-[2-[2-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]tetrazol-5-yl]-4,5-dimethoxyphenyl]-4-oxochromene-2-carboxamide
N-[2-[2-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]tetrazol-5-yl]-4,5-dimethoxyphenyl]-4-oxochromene-2-carboxamide:hydrochloride | [Molecular Formula]
C38H37ClN6O7 | [MOL File]
849675-88-3.mol | [Molecular Weight]
725.2 |
| Hazard Information | Back Directory | [Uses]
Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC50=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC50=35.4nM[1]. | [References]
[1] Bauer F, et al. Interaction of HM30181 with P-glycoprotein at the murine blood-brain barrier assessed with positron emission tomography. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27. DOI:10.1016/j.ejphar.2012.09.013
[2] Oral docetaxel plus encequidar - a phase 1 clinical trial DOI:10.1007/s00280-024-04674-4
[3] Kim TE, et al. Effects of HM30181, a P-glycoprotein inhibitor, on the pharmacokinetics and pharmacodynamics of loperamide in healthy volunteers. Br J Clin Pharmacol. 2014 Sep;78(3):556-64. DOI:10.1111/bcp.12368 |
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