- Balipodect
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- $45.00 / 2mg
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2025-07-09
- CAS:1238697-26-1
- Min. Order:
- Purity: 99.87%
- Supply Ability: 10g
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| | TAK-063 Basic information |
| Product Name: | TAK-063 | | Synonyms: | TAK-063;1-[2-Fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one;Balipodect;TAK 063;TAK063; Pyridone 6[1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one];CS-1534;TAK-063(Balipodect);TAK063, TAK 063, TAK-063, BALIPODECT | | CAS: | 1238697-26-1 | | MF: | C23H17FN6O2 | | MW: | 428.42 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1238697-26-1.mol |  |
| | TAK-063 Chemical Properties |
| Boiling point | 612.3±65.0 °C(Predicted) | | density | 1.37±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:55.0(Max Conc. mg/mL);128.38(Max Conc. mM) | | form | A crystalline solid | | pka | -0.34±0.12(Predicted) | | color | Light yellow to yellow |
| | TAK-063 Usage And Synthesis |
| Description | TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 0.3 nM). It is >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. TAK-063 (0.3 mg/kg) increases cAMP and cGMP levels by 1.3- and 2.14-fold, respectively, in the striatum of mice. It reverses hyperlocomotion induced by PCP (Item Nos. 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 (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats. | | Uses | 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. | | 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[1].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[2]. | | IC 50 | PDE10 | | References | [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(22):9627-43. DOI:10.1021/jm5013648
[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. DOI:10.1124/jpet.114.218552 |
| | TAK-063 Preparation Products And Raw materials |
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