半岛bd体育手机客户端 描述
SAR7334 hydrochloride is a potent and specific inhibitor of TRPC6(IC50 of 7.9 nM).
体外活性
SAR7334 inhibits 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 with an 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. 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.
1333207-63-8
分子式
C21H24Cl3N3O
分子量
440.79
别名
SAR7334 hydrochloride
储存和溶解度
DMSO:100 mg/mL (226.87 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years