| Identification | Back Directory | [Name]
TAK-063 | [CAS]
1238697-26-1 | [Synonyms]
TAK-063
CS-1534
Balipodect
TAK 063;TAK063
TAK-063(Balipodect)
TAK063, TAK 063, TAK-063, BALIPODECT
1-[2-Fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one
4(1H)-Pyridazinone, 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-
Pyridone 6[1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one] | [Molecular Formula]
C23H17FN6O2 | [MDL Number]
MFCD28385852 | [MOL File]
1238697-26-1.mol | [Molecular Weight]
428.42 |
| Chemical Properties | Back Directory | [Boiling point ]
612.3±65.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:55.0(Max Conc. mg/mL);128.38(Max Conc. mM) | [form ]
A crystalline solid | [pka]
-0.34±0.12(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
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 <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 (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats. |
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