中文名 | TRPC6-IN-1 |
英文名 | TRPC6-IN-1 |
别名 | 化合物 T13213 |
英文别名 | TRPC6-IN-1 1-Piperidinecarboxylic acid, 4-[3-(4-fluorophenyl)-7-hydroxy-2-methylpyrazolo[1,5-a]pyrimidin-5-yl]-, ethyl ester |
CAS | 901715-05-7 |
化学式 | C21H23FN4O3 |
分子量 | 398.43 |
密度 | 1.37±0.1 g/cm3(Predicted) |
酸度系数 | 5.46±0.53(Predicted) |
存储条件 | 2-8°C,密封,干燥 |
外观 | 固体 |
体外研究 | TRPC6-IN-1 (compound 4o) rises in the TRPC6 cells in a concentration dependent manner, with a mean EC 50 value of 4.66±0.03 μM, demonstrating a comparable activity of the compound on TRPC6 as the original lead. TRPC6-IN-1 is also tested on HEK293 cells that co-expressed μ opioid receptor (MOR) and TRPC4β, which belongs to a different subgroup of TRPC channels than TRPC3/6/7. Upon stimulation by a μ agonist, these cells show a robust increase in [Ca 2+ ] i . TRPC6-IN-1 also evokes whole-cell currents in HEK293 cells that express human TRPC3. TRPC6-IN-1 elicits concentration dependent current increases in the TRPC7 cells. Different from TRPC6, the currents show some desensitization in the high TRPC6-IN-1 concentrations (10 and 30 μM) at both negative and positive potentials even though the low Ca 2+ (0.1 mM) bath solution is used. Nonetheless, a stepwise increase in the TRPC7 currents is still detected at <10 μM TRPC6-IN-1. |
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