KV2 channel inhibitor-1

• CAT Number: I030207
• CAS Number: 689297-68-5
• Molecular Formula: C20H17ClN4OS
• Molecular Weight: 396.89
• Purity: ≥95%
• Synonyms: 3-(3-chlorophenyl)-N-[2-(1,3-thiazol-4-yl)-3H-benzimidazol-5-yl]butanamide
• InChI: InChI=1S/C20H17ClN4OS/c1-12(13-3-2-4-14(21)8-13)7-19(26)23-15-5-6-16-17(9-15)25-20(24-16)18-10-27-11-22-18/h2-6,8-12H,7H2,1H3,(H,23,26)(H,24,25)
• InChIKey: MRQZOINSVKHDQS-UHFFFAOYSA-N
• SMILES: CC(CC(=O)NC1=CC2=C(C=C1)N=C(N2)C3=CSC=N3)C4=CC(=CC=C4)Cl

KV2 channel inhibitor-1 is a selective KV2 channel inhibitor with IC50s of 0.2 μM and 0.41 μM for KV2.1 and KV2.2, respectively. KV2 channel inhibitor-1 possesses good selectivity over KV1.2 (IC50>10 μM). KV2 channel inhibitor-1 is >10-fold selective over NaV channels and other KV channels and displays weak activity on CaV channels[1].
KV2 channel inhibitor-1 (compound A1; 0.3, 1, 3 μM; 0-3000s) inhibits the KV current in rat insulinoma INS-1 cells. KV2 channel inhibitor-1 blocks INS-1 KV current an average of 71% at 0.3 μM and 84% at 3 μM[1].

Reference

[1]. James Herrington, et al. Identification of novel and selective Kv2 channel inhibitors. Mol Pharmacol. 2011 Dec;80(6):959-64.
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