TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC 50 of 4.66 μM. In Vitro 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 IC50& Target:EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3)
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TRPC6-IN-1
CAS number：901715-05-7(DMSO) molecular formula：C21H23FN4O3
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 901715-05-7(DMSO) | molecular formula | C21H23FN4O3 |
| molecular weight | 398.43 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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