893990-34-6

893990-34-6 structure

Name: VU 0240551
Chemical Name: N-(4-methyl-1,3-thiazol-2-yl)-2-(6-phenylpyridazin-3-yl)sulfanylacetamide
CAS Number: 893990-34-6
Molecular Formula: C₁₆H₁₄N₄OS₂
Molecular Weight: 342.43900
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
Create Date: 2017-01-27 12:22:53
Modify Date: 2024-01-03 19:12:01
VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).IC50 value: 560 nM [1]Target: K-Cl cotransporter(KCC2)VU 0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. VU 0240551 also inhibits hERG and L-type Ca2+ channels [1]. Herein we report the discovery and SAR of an improved novel antagonist (VU0463271) of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC(50) 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 [2].

Name	N-(4-methyl-1,3-thiazol-2-yl)-2-(6-phenylpyridazin-3-yl)sulfanylacetamide
Synonyms	VU 0240551

Description	VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).IC50 value: 560 nM [1]Target: K-Cl cotransporter(KCC2)VU 0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. VU 0240551 also inhibits hERG and L-type Ca2+ channels [1]. Herein we report the discovery and SAR of an improved novel antagonist (VU0463271) of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC(50) 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 [2].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Research Areas >> Others
References	[1]. Delpire E, et al. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. [2]. Delpire E, et al. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4532-5.

RIDADR	NONH for all modes of transport