NS1652 是可逆阴离子电导抑制剂,在人和小鼠的红细胞中,可以抑制氯离子通道,IC50值为 1.6 μM。
产品描述
NS1652 is an anion conductance inhibitor. NS1652 blocks chloride channel has an IC50 of 1.6 μM in human and mouse red blood cells.
体外活性
NS1652 (20 μM) fully and reversibly inhibits the red cell Cl-conductance. NS1652 effectively inhibits the chloride conductance (IC50, 1.6 μM) in human and mouse red blood cells, but only weakly inhibits VRAC (IC50, 125 μM) in HEK293 cells. NS1652 markedly blocks the NO production (IC50: 3.1 μM in BV2 cells). NS1652 also down-regulates iNOS expression at 3 μM and fully abolishes at 10 μM in BV2 cells. NS1652 (0, 1.0, 3.3, 10, and 20 μM) induces increasing hyperpolarization due to inhibition of the chloride conductance in normal erythrocytes. NS1652 lowers the net KCl loss from deoxygenated sickle cells from about 12 mM cells/h to about 4 mM cells/h [1][2].
体内活性
In mice, NS1652 (50 mg/kg, i.v.) blocks murine erythrocyte Cl- conductance by >90%[2].
Cas No.
1566-81-0
分子式
C15H11F3N2O3
分子量
324.25
储存和溶解度
DMSO:4.9 mg/mL (15.11 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years