产品描述: | SAR7334是一种新型,高效且可生物利用的TRPC6通道抑制剂。SAR7334在膜片钳实验中阻断了TRPC6电流,IC50为7.9 nM |
靶点: |
TPRC6(Cell-free assay):7.9nM;TRP/TRPVChannel |
体外研究: |
SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected..SAR7334 suppresses TRPC6-dependent acute HPV in isolated perfused lungs from mice |
体内研究: |
Pharmacokinetic studies of SAR7334 demonstrates that the compound was suitable for chronic oral administration. In an initial short-term study, SAR7334 does not change mean arterial pressure in spontaneously hypertensive rats (SHR) |
细胞实验: |
Cell lines: HEK cells Concentrations: '-- Incubation Time: 10min Method: The cells are rinsed and incubated with standard extracellular solution supplemented with different concentrations of the test compound or vehicle for 10 min. |
动物实验: |
Animal Models: Sprague Dawley rat Dosages: 10mg/kg Administration: oral |
参考文献: |
1. Maier T,et al.Discovery and pharmacological characterization of a novel potent inhibitor of diacylglycerol-sensitive TRPC cation channels. Br J Pharmacol.2015;172(14):3650-60 |
溶解性: |
Soluble in DMSO、Ethanol |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.718 ml |
13.592 ml |
27.183 ml |
5 mM |
0.544 ml |
2.718 ml |
5.437 ml |
10 mM |
0.272 ml |
1.359 ml |
2.718 ml |
50 mM |
0.054 ml |
0.272 ml |
0.544 ml |
|
注意: |
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