产品描述
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, slowing of deactivation, reduction of inactivation, and abbreviates atrial and ventricular repolarization[1][2].
体外活性
A-935142 shortens the action potential duration (APD90) in guinea pig atrial tissue, canine cardiac Purkinje fibers[1], and cardiac action potentials. A-935142 (60μM) increases both outward and inward K(+) current as well as the slope conductance of the linear portion of the fully activated I-V relation. A-935142 enhances the amplitude of the hERG current in a concentration- and voltage-dependent manner. A-935142 significantly reduces the time constants (tau) of hERG channel activation at two example voltages (-10 mV: tau=100+/-17 ms vs. 164+/-24 ms, n=6, P<0.01; +30 mV: tau=16.7+/-1.8 ms vs. 18.9+/-1.8 ms, n=5, P<0.05) and shifts the voltage-dependence for hERG activation in the hyperpolarizing direction by 9 mV[2].
Cas No.
1031335-85-9
分子式
C18H19F3N2O2
分子量
352.35
别名
A-935142
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years