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Medchemexpress LLC VU0463271 | 1391737-01-1 | 99.8% | 382.50 | 10 MG
Supplier: Medchemexpress LLC HY11011050MG
VU0463271 is a selective and potent KCC2 antagonist. It demonstrates high selectivity over NKCC1 and no activity against a broad panel of GPCRs, ion channels, and transporters. In vitro, it is rapidly cleared. In vivo studies in rats show it is a moderate-to-high clearance compound.
- IC50 of 61 nM for KCC2.
- >100-fold selectivity over NKCC1.
- No activity against GPCRs, ion channels, and transporters.
- Rapidly cleared in vitro.
- Significantly increased firing rates in Drosophila CNS.
- Moderate-to-high clearance (CL=57 mL/min/kg) in rats after intravenous administration.
- Low volume of distribution at steady state (Vss 0.4 L/kg) in rats.
- Relatively short t1/2 (9 min) in rats.
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