NNC 55-0396

NNC 55-0396 is a selective inhibitor of T-type calcium channels that blocks Cav3.1 in stably expressing HEK293 cells (IC50 = 6.8 µM) with no discernible effect on high voltage-activated (L-type) channels in INS-1 cells up to a concentration of 100 µM. NNC 55-0396 suppresses tremor in two murine models, the GABAA alpha1-null (20 mg/kg) and harmaline-induced (12.5 mg/kg) tremor models, and was better tolerated than mibefradil (Cay-15037). In arterial smooth muscle cells, NCC 55-0396 (IC50 = 80 nM) inhibits voltage-dependent K+ channels but does not affect their voltage sensitivity. NNC 55-0396 (1-5 µM) also suppresses angiogenesis in vitro by inhibiting hypoxia-inducible factor-1alpha activity, and it slows tumor growth of flank xenografts of U87MG cells in mice when administered at 20 mg/kg.Formal Name: cyclopropanecarboxylic acid, (1S,2S)-2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl ester, dihydrochloride. CAS Number: 357400-13-6. Molecular Formula: C30H38FN3O2 . 2HCl. Formula Weight: 564.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, Ethanol: 30 mg/mL, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/mL. SMILES: FC1=CC(CC[C@@](CCN(C)CCCC2=NC(C=CC=C3)=C3N2)(OC(C4CC4)=O)[C@H]5C(C)C)=C5C=C1.Cl.Cl. InChi Code: InChI=1S/C30H38FN3O2.2ClH/c1-20(2)28-24-13-12-23(31)19-22(24)14-15-30(28,36-29(35)21-10-11-21)16-18-34(3)17-6-9-27-32-25-7-4-5-8-26(25)33-27,,/h4-5,7-8,12-13,19-21,28H,6,9-11,14-18H2,1-3H3,(H,32,33),2*1H/t28-,30-,,/m0../s1. InChi Key: BCCQNBXHUMKLFW-HNQRYHMESA-N.