SAR7334 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SAR7334 hydrochloride 是一种有效的 TRPC6 特异性抑制剂，能够抑制 TRPC6 电流，IC50 值为 7.9 nM。

SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.

SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca2+ influx into cells with IC50s of 9.5, 282 and 226?nM, 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. SAR7334 (1 μM) has negligible effect on SOCE. SAR7334 dose-dependently reduces TRPC6 currents with an IC50 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).

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1333207-63-8

440.79

C21H24Cl3N3O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (226.87 mM; 超声助溶 ) H2O 中的溶解度 : 50 mg/mL (113.43 mM; 超声助溶)

Cl.Cl.N[C@@H]1CCCN(C1)[C@@H]1Cc2ccccc2[C@H]1Oc1ccc(cc1Cl)C#N

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(-20℃)

With Ice Pack

≥ 2 years