A potent inhibitor of PDE10A
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TAK-063

Item No. 22208

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMSO: >1 mg/mlEthanol: >1 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 0.3 nM).1 It is >15,000-fold selective for PDE10A over other PDEs and exhibits <50% inhibition at 91 receptors, ion channels, and enzymes at a concentration of 10 μM. TAK-063 (0.3 mg/kg) increases cAMP and cGMP levels by 1.3- and 2.14-fold, respectively, in the striatum of mice. It reverses hyperlocomotion induced by PCP (Item Nos. 14276 | 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 (Item No. 10009019) (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats.2

    WARNING This product is not for human or veterinary use.