VU 0240551

• CAT Number: I005350
• CAS Number: 893990-34-6
• Molecular Formula: C16H14N4OS2
• Molecular Weight: 342.44
• Purity: ≥95%
• Target: Potassium Channel
• Solubility: 10 mM in DMSO
• Storage: 2-8°C
• IC50: 560 nM
• IUPAC Name: N-(4-methyl-1,3-thiazol-2-yl)-2-(6-phenylpyridazin-3-yl)sulfanylacetamide
• InChI: InChI=1S/C16H14N4OS2/c1-11-9-23-16(17-11)18-14(21)10-22-15-8-7-13(19-20-15)12-5-3-2-4-6-12/h2-9H,10H2,1H3,(H,17,18,21)
• InChIKey: WJRWSLORVIHRNX-UHFFFAOYSA-N
• SMILES: CC1=CSC(=N1)NC(=O)CSC2=NN=C(C=C2)C3=CC=CC=C3

VU0240551 is an effective inhibitor of neuronal K-Cl cotransporter KCC2 ( IC50 = 560nM ), which is selective compared with NKCC1. VU024055Chemicalbook1also inhibited hERG and L-type Ca2 + channels. VU0240551 attenuates GABA-induced P cell hyperpolarization, positively shifts the GABA reversal potential of P cells, and enhances P cell synaptic transmission.

Reference

[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.