TRPC6-IN-1 (C09-1182-368)

TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC 50 of 4.66 μM.In VitroTRPC6-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3). Specifications and Purity: 99%. Molecular Formula: C21H23FN4O3. Molecular Weight: 398.43. PubChem CID: 5308428. Isomeric SMILES: CCOC(=O)N1CCC(CC1)C2=CC(=O)N3C(=N2)C(=C(N3)C)C4=CC=C(C=C4)F.