TAK-063

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TAK-063 (Balipodect) 是一种高效、选择性、口服活性的 PDE10A 抑制剂，IC50 为 0.3 nM。

TAK-063 (Balipodect) is a highly potent, selective, orally active PDE10A inhibitor with IC50 of 0.3 nM, displays >15,000-fold selectivity over other PDE subtypes; increases cAMP and cGMP levels in the rodent striatum and upregulates phosphorylation levels of key substrates of cAMP- and cGMP-dependent protein kinases, strongly suppresses MK-801-induced hyperlocomotion in rodents (0.3 and 1 mg/kg p.o), improves cognitive functions associated with schizophrenia in rodent models,Schizophrenia Phase 2 Discontinued(In Vivo):Balipodect (TAK-063) has excellent selectivity (>15000-fold selectivity over other PDEs), and favorable pharmacokinetics, including high brain penetration, in mice. Oral administration of Balipodect (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.Balipodect (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. Balipodect (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. Balipodect (TAK-063) did not affect plasma prolactin or glucose levels at doses up to 3 mg/kg, p.o. Balipodect (TAK-063) at 3 mg/kg, p.o., elicited a weak cataleptic response compared with haloperidol and olanzapine.

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Balipodect (TAK-063) has excellent selectivity (>15000-fold selectivity over other PDEs), and favorable pharmacokinetics, including high brain penetration, in mice. Oral administration of Balipodect (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.Balipodect (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. Balipodect (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. Balipodect (TAK-063) did not affect plasma prolactin or glucose levels at doses up to 3 mg/kg, p.o. Balipodect (TAK-063) at 3 mg/kg, p.o., elicited a weak cataleptic response compared with haloperidol and olanzapine.

TAK063 | Balipodect

Angiogenesis

PDE

PDE10A

Neurological Disease

Schizophrenia

1238697-26-1

428.4185

C23H17FN6O2

>98% (HPLC)

10 mM in DMSO

O=C1C(C2=CC=NN2C3=CC=CC=C3)=NN(C4=CC=C(N5N=CC=C5)C=C4F)C=C1OC

4(1H)-Pyridazinone, 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-

(-20℃)

With Ice Pack

≥ 2 years