| Bioactivity | Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. | ||||||||||||
| Invitro | Encequidar (HM30181; HM30181A) 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, Encequidar (HM30181): 13.1±2.3 nM) [1]. Encequidar (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[2]. | ||||||||||||
| 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]. | ||||||||||||
| Name | Encequidar | ||||||||||||
| CAS | 849675-66-7 | ||||||||||||
| Formula | C38H36N6O7 | ||||||||||||
| Molar Mass | 688.73 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. |