| Identification | Back Directory | [Name]
HM 30181A | [CAS]
849675-66-7 | [Synonyms]
HM30181
HM 30181A
HM30181;HM30181A
HM30181(Encequidar)
4H-1-Benzopyran-2-carboxamide, N-[2-[2-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-2H-tetrazol-5-yl]-4,5-dimethoxyphenyl]-4-oxo- | [Molecular Formula]
C38H36N6O7 | [MOL File]
849675-66-7.mol | [Molecular Weight]
688.73 |
| Chemical Properties | Back Directory | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF:30.0(Max Conc. mg/mL);43.56(Max Conc. mM) | [form ]
A crystalline solid | [pka]
7.95±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. | [in vivo]
PET scans with the Pgp substrate (R)-[11C]NSC 657799 in FVB wild-type mice pretreated i.v. with Encequidar (HM30181) (10 or 21 mg/kg) failes to show significant increases in (R)-[11C]NSC 657799 brain uptake compared with vehicle treated animals[1]. Encequidar (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. Encequidar (HM30181) increases the oral bioavailability of co-administered NSC 125973 by more than 12 times in rats[2]. | [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] 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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