| Description | SAR7334 hydrochloride is a potent and specific inhibitor of TRPC6(IC50 of 7.9 nM). |
| In vitro | 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]. |
| In vivo | 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]. |
| Target activity | TRPC6 current:7.9 nM |
| molecular weight | 440.79 |
| Molecular formula | C21H24Cl3N3O |
| CAS | 1333207-63-8 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 100 mg/mL (226.87 mM), Sonication is recommended. |
| References | 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. |