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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-TAK-063
TAK-063

Chemical Structure : TAK-063

CAS No.: 1238697-26-1

TAK-063 (TAK063, Balipodect)

货号: PC-43051Not For Human Use, Lab Use Only.

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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
TAK-063 increases cAMP and cGMP levels in the rodent striatum and upregulates phosphorylation levels of key substrates of cAMP- and cGMP-dependent protein kinases.
TAK-063 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,

物理化学性质&存储条件

分子量 428.4185
分子式 C23H17FN6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Kunitomo J, et al. J Med Chem. 2014 Nov 26;57(22):9627-43.

2. Suzuki K, et al. J Pharmacol Exp Ther. 2015 Mar;352(3):471-9.

3. Shiraishi E, et al. J Pharmacol Exp Ther. 2016 Mar;356(3):587-95.

4. Suzuki K, et al. Neuropsychopharmacology. 2016 Aug;41(9):2252-62.

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