TAK-063

TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A, IC50 = 0.3 nM). It is >15,000-fold selective for PDE10A over other PDEs and exhibits 14276, Cay-ISO60194) with a minimum effective dose (MED) of 0.3 mg/kg, p.o., in wild-type mice but has no effect in PDE10A knockout mice at doses up to 1 mg/kg. TAK-063 also reverses hyperlocomotion induced by (+)-MK-801 (Cay-10009019) (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats.Formal Name: 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-4(1H)-pyridazinone. CAS Number: 1238697-26-1. Molecular Formula: C23H17FN6O2. Formula Weight: 428.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: >1 mg/ml, Ethanol: >1 mg/ml. lambdamax: 247, 272, 338 nm. SMILES: O=C1C(C2=CC=NN2C3=CC=CC=C3)=NN(C4=CC=C(N5C=CC=N5)C=C4F)C=C1OC. InChi Code: InChI=1S/C23H17FN6O2/c1-32-21-15-29(19-9-8-17(14-18(19)24)28-13-5-11-25-28)27-22(23(21)31)20-10-12-26-30(20)16-6-3-2-4-7-16/h2-15H,1H3. InChi Key: KVHRYLNQDWXAGI-UHFFFAOYSA-N.