VU0463271 是一种有效的、特异性的 KCC2 拮抗剂，其 IC50 为 61 nM，特异性是密切相关的 Na-K-2Cl 协同转运蛋白 1 (NKCC1) 的 100 倍以上，在更大的 GPCR、离子通道和转运蛋白面板中没有活性。

VU0463271 is a potent and selective antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels, and transporters.

VU0463271 is also found rapidly cleared in vitro[1]. VU0463271 is applied to the transected CNS preparation and resulted in a significant increase in firing rates of the Drosophila CNS with 1 μM VU0463271 resulting in a peak firing rate that was a 2.7- and 2.5-fold increase over baseline firing rate for OR and rdl strains, respectively[2].

VU0463271(1 mg/kg; i.v.) is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg). The low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo[

1391737-01-1

C19H18N4OS2

382.5

N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide

DMSO:20 mg/mL (52.29 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years