1333210-07-3
1333210-07-3 结构式
基本信息
TRCP6-IN-1
TRCP6 inhibitor
4-(((1R,2R)-2-((R)-3-Aminopiperidin-1-yl)-2,3-dihydro-1H-inden-1-yl)oxy)-3-chlorobenzonitrile
Benzonitrile, 4-[[(1R,2R)-2-[(3R)-3-aMino-1-piperidinyl]-2,3-dihydro-1H-inden-1-yl]oxy]-3-chloro-
物理化学性质
常见问题列表
| Target | Value |
|
TPRC6
(Cell-free assay) | 7.9nM |
SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca 2+ influx into cells with IC 50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca 2+ entry is not affected. SAR7334 (1 μM) results in a major block of the Ang II-evoked calcium influx in the podocytes. SAR7334 (1 μM) has negligible effect on SOCE. SAR7334 dose-dependently reduces TRPC6 currents with an IC 50 of 7.9 nM. SAR7334 (100 nM) substantially reduces TRPC6 currents.
SAR7334 (10 mg/kg, p.o.) suppresses TRPC6-dependent acute HPV in isolated perfused lungs from mice. 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).