KR30031

KR30031, a Verapamil (HY-14275) analog, is an orally active P-glycoprotein (P-gp) inhibitor. KR30031 enhances the cytotoxicity of anticancer agents by inhibiting P-gp with fewer cardiovascular adverse effects. KR30031 can be used to study multidrug resistance (MDR) reversal in cancer^[1][2]. In Vitro:KR30031 (0.01-100 μM) produces concentration-dependent relaxation of aorta precontracted with 60 mM KCl, with an EC₅₀ of 9.14 μM^[1].
KR30031 (0.0001-100 mM) induces a concentration-dependent decrease in left ventricular pressure (LVP) of isolated hearts, with an EC₅₀ of 11.6 mM; it also causes a concentration-dependent decrease in heart rate (HR) of isolated hearts^[1].
KR30031 (0.3-10.0 μM, 72 h) enhances Paclitaxel (HY-B0015)-induced cytotoxicity to HCT15/CL02 and MES-SA/DX5 cells with high P-glycoprotein expression, with IC₅₀ values of 3.20 μM and 7.63 μM, respectively^[1].
KR30031 (0.3-100 μM, 72 h) shows intrinsic cytotoxicity to HCT15/CL02 and MES-SA/DX5 cells only at 100 μM^[1].
KR30031 (25 μM) increases apical-to-basolateral transport of Paclitaxel in Caco-2 cell monolayer, with potency equal to Verapamil (HY-14275)^[2].
In Vivo:KR30031 (administered intravenously at 5-min intervals 40 minutes after surgery) produces a dose-dependent reduction in mean arterial pressure (MAP) in anesthetized rats, with an ED₂₀ of 0.842 mg/kg and dose-dependently decreases HR, with an ED₂₀ of 2.588 mg/kg^[1].