TAK-994

An orexin receptor 2 agonist, selectively induces calcium mobilization in CHO-K1 cells expressing human OX2R over those expressing OX1R (EC50s = 0.019 and 14 µM, respectively), selective for OX2R over a panel of 106 enzymes, receptors, and ion channels at 10 µM, increases wakefulness time and wakefulness episode duration and inhibits chocolate-induced cataplexy-like episodes during the active phase in a model of narcolepsy using mice with orexin neurons ablated by ataxin-3 expression, increases wakefulness time but does not affect OXA or OXB CSF levels during the sleep phase in cynomolgus monkeys at 10 mg/kg. Formulation: A solid. InChI: InChI=1S/C22H25F3N2O4S/c1-22(2,29)21(28)27-8-7-18(26-32(3,30)31)19(27)11-13-5-4-6-17(20(13)25)14-9-15(23)12-16(24)10-14/h4-6,9-10,12,18-19,26,29H,7-8,11H2,1-3H3/t18-,19-/m0/s1. InChIKey: VOSAWOSMGPKQEQ-OALUTQOASA-N. SMILES: CC(C)(O)C(N(CC[C@@H]1NS(=O)(C)=O)[C@H]1CC2=C(C(C3=CC(F)=CC(F)=C3)=CC=C2)F)=O