SAR7334 是TRPC6特异性抑制剂,抑制 TRPC6 电流的IC50为 7.9 nM。
产品描述
SAR7334 is a potent and specific inhibitor of TRPC6(IC50 of 7.9 nM).
体外活性
SAR7334 is an inhibitor of TRPC6, TRPC3 and TRPC7-mediated Ca2+ influx into cells(IC50s of 9.5, 282 and 226?nM)[1][2][3], whereas TRPC4 and TRPC5-mediated Ca2+ entry is not affected. SAR7334 (1?μM) results in a major block of the Ang II-evoked calcium influx in the podocytes[1].SAR7334 dose-dependently reduces TRPC6 currents (IC50 of 7.9?nM). SAR7334 (100?nM) substantially reduces TRPC6 currents[3].
体内活性
In isolated perfused lungs from mice, SAR7334 (10?mg/kg, p.o.) inhibits TRPC6-dependent acute HPV . SAR7334 demonstrates that it is suitable for chronic oral administration. In an initial short-term study, SAR7334 does not change mean arterial pressure in spontaneously hypertensive rats (SHR)[3].
Cas No.
1333210-07-3
分子式
C21H22ClN3O
分子量
367.87
别名
TRCP6-IN-1
储存和溶解度
DMSO:350 mg/mL (951.42 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years