Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.

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) .
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . 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.  [Content Brief]

  . 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.  [Content Brief]