TRPC6 inhibitor |
| Catalog No.GC13218 |
TRPC6 inhibitor is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1333207-63-8
Sample solution is provided at 25 µL, 10mM.
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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[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 (1 μM) has negligible effect on SOCE[2]. SAR7334 dose-dependently reduces TRPC6 currents with an IC50 of 7.9 nM. SAR7334 (100 nM) substantially reduces TRPC6 currents[3].
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)[3].
[1]. Ilatovskaya DV, et al. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299.
[2]. Chauvet S, et al. Pharmacological Characterization of the Native Store-Operated Calcium Channels of Cortical Neurons from Embryonic Mouse Brain. Front Pharmacol. 2016 Dec 12;7:486.
[3]. Maier T, et al. Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol. 2015 Jul;172(14):3650-60.
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