A potent inhibitor of PDE10A (IC50 = 0.3 nM); >15

TAK-063 – 50 mg

Brand:
Cayman
CAS:
1238697-26-1
Storage:
-20
UN-No:
Non-Hazardous - /

TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 0.3 nM).{38458} It is >15,000-fold selective for PDE10A over other PDEs and exhibits 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.{38459}  

 

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Description

A potent inhibitor of PDE10A (IC50 = 0.3 nM); >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; increases cAMP and cGMP levels by 1.3- and 2.14-fold, respectively, in the striatum of mice when administered at a dose of 0.3 mg/kg; reverses PCP-induced hyperlocomotion (MED = 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; reverses (+)-MK-801-induced hyperlocomotion (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

Synonyms: 

Molecular weight: 428.4

CAS: 1238697-26-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Neuroscience|Behavioral Neuroscience

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