Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC 50 of 61 nM [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,530.00 | |
50 mg | 10-14 weeks | $ 1,997.00 | |
100 mg | 10-14 weeks | $ 2,995.00 |
Description | VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC 50 of 61 nM [1]. |
In vitro | VU0463271 is a highly effective antagonist targeting the neuronal-specific potassium-chloride cotransporter 2 (KCC2), demonstrating significant potency with an IC50 value of 61 nM. It exhibits over 100-fold selectivity against the closely related Na-K-2Cl cotransporter 1 (NKCC1) and shows no activity across a wide range of G-protein coupled receptors (GPCRs), ion channels, and transporters. VU0463271 is also characterized by rapid clearance in vitro [1]. When applied to transected CNS preparations, VU0463271 significantly elevates the firing rates in the Drosophila CNS. Concentrations of 1 μM of VU0463271 notably increased the peak firing rate by 2.7- and 2.5-fold over the baseline for OR and rdl strains, respectively [2]. Furthermore, doses ranging from 10-100 nM led to an approximate 20% reduction in CNS firing frequency in a minority of the preparations [2]. |
In vivo | VU0463271 exhibits moderate-to-high clearance (CL=57 mL/min/kg) in rats when administered intravenously at a dose of 1 mg/kg. Its low steady-state volume of distribution (Vss 0.4 L/kg), combined with its clearance rate, results in a relatively short half-life (t1/2) of 9 minutes in vivo [1]. |
Molecular Weight | 387 |
Formula | C19H20N4O2S2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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VU0463271 quarterhydrate inhibitor inhibit