Encequidar (HM30181; HM30181A) is a potent and selective inhibitor ofP-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)^[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].

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].

688.73

Solid

C₃₈H₃₆N₆O₇

849675-66-7

Room temperature in continental US; may vary elsewhere.

DMSO : 2.4 mg/mL(3.48 mM;Need ultrasonic)

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