CAS NO: | 901715-05-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel(TRPC6)inhibitor, with anEC50of 4.66 μM. | ||||||||||||||||
IC50& Target | EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3)[1]. | ||||||||||||||||
体外研究 (In Vitro) | TRPC6-IN-1 (compound 4o) rises in the TRPC6 cells in a concentration dependent manner, with a mean EC50value 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-expressedμopioid receptor (MOR) and TRPC4β, which belongs to a different subgroup of TRPC channels than TRPC3/6/7. Upon stimulation by aμagonist, these cells show a robust increase in [Ca2+]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 Ca2+(0.1 mM) bath solution is used. Nonetheless, a stepwise increase in the TRPC7 currents is still detected at<10 μm trpc6-in-1[1]. | ||||||||||||||||
分子量 | 398.43 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H23FN4O3 | ||||||||||||||||
CAS 号 | 901715-05-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(250.99 mM;Need ultrasonic) 配制储备液
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