Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TRPC3/6-IN-1 is a highly potent and selective inhibitor that specifically blocks the activity of the canonical transient receptor channels TRPC3 and TRPC6. It exhibits a significant blocking potency against the human isoforms hTRPC3 and hTRPC6, with IC50 values of 1260 nM and 500 nM, respectively. This compound, TRPC3/6-IN-1, is particularly valuable for conducting research on chronic models of heart failure [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 35 days | $ 83.00 | |
5 mg | 35 days | $ 268.00 | |
10 mg | 35 days | $ 450.00 | |
25 mg | 35 days | $ 918.00 |
Description | TRPC3/6-IN-1 is a highly potent and selective inhibitor that specifically blocks the activity of the canonical transient receptor channels TRPC3 and TRPC6. It exhibits a significant blocking potency against the human isoforms hTRPC3 and hTRPC6, with IC50 values of 1260 nM and 500 nM, respectively. This compound, TRPC3/6-IN-1, is particularly valuable for conducting research on chronic models of heart failure [1]. |
In vitro | TRPC3/6-IN-1 exhibits blocking activity against hTRPC3 and hTRPC6, achieving half-maximal inhibitory concentrations (IC50) of 1260 nM and 500 nM, respectively [1]. |
In vivo | TRPC3/6-IN-1 (compound 3) demonstrates favorable pharmacokinetics in rats, as evidenced by its pharmacokinetic parameters. Administered intravenously at a dose of 0.93 mg/kg, it achieves a maximum concentration (Cmax) of 250 ng/ml and is cleared from the body at a rate of 120 ml/min/kg. The mean residence time (MRT) is 0.3 hours, with a normalized area under the curve (DNAUC) of 0.14 h kg/L, indicating an oral bioavailability (~F) of approximately 1%. |
Molecular Weight | 365.45 |
Formula | C20H19N3O2S |
CAS No. | 736945-96-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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TRPC3/6-IN-1 736945-96-3 inhibitor inhibit