TAK-063 supplier|TAK063|DC Chemicals

TAK-063 supplier|TAK063|DC Chemicals
DC Chemicals provides TAK-063, other names: TAK 063，TAK063, cas: 1238697-26-1. In stock.

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TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.

TAK-063, other names: TAK 063，TAK063, cas: 1238697-26-1, Molecule formular: C23H17FN6O2, Molecule Weight: 428.42, Chemical name: 1-(2-fluoro-4-(1H-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one

TAK-063 has potent inhibitory activity (IC50 = 0.30 nM), excellent selectivity (>15000-fold selectivity over other PDEs), and favorable pharmacokinetics, including high brain penetration, in mice. Oral administration of TAK-063 to mice elevated striatal 3',5'-cyclic adenosine monophosphate (cAMP) and 3',5'-cyclic guanosine monophosphate (cGMP) levels at 0.3 mg/kg and showed potent suppression of phencyclidine (PCP)-induced hyperlocomotion at a minimum effective dose (MED) of 0.3 mg/kg [1]. TAK-063 at 0.3 and 1 mg/kg, p.o., increased cAMP and cGMP levels in the rodent striatum and upregulated phosphorylation levels of key substrates of cAMP-dependent and cGMP-dependent protein kinases. TAK-063 at 0.3 and 1 mg/kg, p.o., strongly suppressed MK-801-induced hyperlocomotion that is often used as a predictive model for antipsychotic-like activity in rodents. TAK-063 did not affect plasma prolactin or glucose levels at doses up to 3 mg/kg, p.o. TAK-063 at 3 mg/kg, p.o., elicited a weak cataleptic response compared with haloperidol and olanzapine  For the detailed information of TAK-063, the solubility of TAK-063 in water, the solubility of TAK-063 in DMSO, the solubility of TAK-063 in PBS buffer, the animal experiment (test) of  TAK-063, the cell expriment (test) of TAK-063, the in vivo, in vitro and clinical trial test of TAK-063, the EC50, IC50,and affinity,of TAK-063, Please contact DC Chemicals.