品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S80213-1mg	98%	￥50.00元	10	-	-	-
源葉(MedMol)	S80213-2mg	98%	￥80.00元	10	-	-	-
源葉(MedMol)	S80213-5mg	98%	￥110.00元	7	-	-	-
源葉(MedMol)	S80213-10mg	98%	￥190.00元	5	-	-	-
源葉(MedMol)	S80213-25mg	98%	￥390.00元	3	-	-	-
源葉(MedMol)	S80213-50mg	98%	￥600.00元	預(yù)計交期：2-3天	-	-	-
源葉(MedMol)	S80213-100mg	98%	￥1020.00元	預(yù)計交期：2-3天	-	-	-

產(chǎn)品介紹

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

產(chǎn)品描述： Balipodect (TAK-063) is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs

靶點： IC50: 0.3 nM (PDE10A);PDE

體內(nèi)研究：
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

參考文獻：
1. Kunitomo J, et al. Discovery of 1-[2-Fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a Highly Potent, Selective, and Orally Active Phosphodiesterase 10A (PDE10A) Inhibitor. J Med Chem. 2014 Nov 26;57 2. Suzuki K, et al. In Vivo Pharmacological Characterization of TAK-063, a Potent and Selective Phosphodiesterase 10A Inhibitor with Antipsychotic-Like Activity in Rodents. J Pharmacol Exp Ther. 2014 Dec 18. pii: jpet.114.218552.

溶解性： soluble in DMSO

保存條件： -20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.334 ml	11.671 ml	23.342 ml
5 mM	0.467 ml	2.334 ml	4.668 ml
10 mM	0.233 ml	1.167 ml	2.334 ml
50 mM	0.047 ml	0.233 ml	0.467 ml

注意：

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參考文獻

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