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TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $1,980 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks | 6-8 weeks |
| Description | TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM). |
| Targets&IC50 | TRPC7: 1.13 μM , TRPC3: 4.66 μM, TRPC3:(EC50)0.45 μM |
| In vitro | In the TRPC6 cells, TRPC6-IN-1 rises in a concentration dependent manner(EC50 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.In HEK293 cells . TRPC6-IN-1 also evokes whole-cell currents 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. |
| Molecular Weight | 398.43 |
| Formula | C21H23FN4O3 |
| Cas No. | 901715-05-7 |
| Smiles | CCOC(=O)N1CCC(CC1)c1cc(O)n2nc(C)c(-c3ccc(F)cc3)c2n1 |
| Relative Density. | 1.37 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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