Size | Price | Stock |
---|---|---|
5mg | $480 | In-stock |
10mg | $800 | In-stock |
25mg | $1700 | In-stock |
50mg | $2800 | In-stock |
100mg | $4200 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-101547 |
M.Wt: | 398.43 |
Formula: | C21H23FN4O3 |
Purity: | >98 % |
Solubility: | DMSO : 100 mg/mL (250.99 mM; Need ultrasonic) |
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM. IC50 & Target: EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3)[1]. In Vitro: TRPC6-IN-1 (compound 4o) rises in the TRPC6 cells in a concentration dependent manner, with a mean EC50 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 [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].
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