Crinecerfont

A CRF1 antagonist (Ki = 1.9 nM), selective for CRF1 over CRF2alpha and a panel of 125 receptors, transporters, ion channels, and enzymes at 10 µM, inhibits CRF-induced cAMP production in Y79 cells (IC50 = 3 nM) and CRF-induced ACTH secretion in AtT-20 cells at 3, 30, and 100 nM, prevents restraint stress-induced increases in plasma ACTH levels in rats at 10 mg/kg, p.o., increases punished responding in the Vogel punished drinking task, indicating anxiolytic-like activity, in mice and decreases immobility time in the forced swim test in rats, decreases cumulative weight gain and increases protein gain in fa/fa obese but not lean rats at 30 mg/kg. SMILES: ClC(C=C(C(C)=C1)OC)=C1C2=C(C)SC(N([C@H](C3=CC(F)=C(C=C3)C)CC4CC4)CC#C)=N2. InChi Code: InChI=1S/C27H28ClFN2OS/c1-6-11-31(24(13-19-8-9-19)20-10-7-16(2)23(29)14-20)27-30-26(18(4)33-27)21-12-17(3)25(32-5)15-22(21)28/h1,7,10,12,14-15,19,24H,8-9,11,13H2,2-5H3/t24-/m0/s1. InChi Key: IEAKXXNRGSLYTQ-DEOSSOPVSA-N