ChemicalBook > CAS DataBase List > TAK-063

TAK-063

TAK-063 Structure
TAK-063
  • CAS No.1238697-26-1
  • Chemical Name:TAK-063
  • CBNumber:CB62735539
  • Molecular Formula:C23H17FN6O2
  • Formula Weight:428.42
  • MOL File:1238697-26-1.mol
TAK-063 Property
  • 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
  • FDA UNII 6650W303H0
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338

TAK-063 Chemical Properties,Usage,Production

  • 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
Raw materials
Preparation Products
TAK-063 Suppliers
Global(92)Suppliers
  • Supplier：
    career henan chemical co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：factory@coreychem.com
  • Country：China
  • ProdList：29808
  • Advantage：58
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：+1-781-999-5354<br/>+1-00000000000
  • Email：marketing@targetmol.com
  • Country：United States
  • ProdList：32159
  • Advantage：58
  • Supplier：
    InvivoChem
  • Tel：+1-708-310-1919<br/>+1-13798911105
  • Email：sales@invivochem.cn
  • Country：United States
  • ProdList：6391
  • Advantage：58
  • Supplier：
    LEAPCHEM CO., LTD.
  • Tel：+86-852-30606658
  • Email：market18@leapchem.com
  • Country：China
  • ProdList：43340
  • Advantage：58
  • Supplier：
    Aladdin Scientific
  • Tel：
  • Email：tp@aladdinsci.com
  • Country：United States
  • ProdList：57505
  • Advantage：58
TAK-063 Spectrum
1238697-26-1, TAK-063Related Search:
  • Inhibitors
  • 化学试剂
  • 药靶配体
  • 小分子抑制剂
  • 抑制剂
  • 小分子抑制剂，天然产物
  • C23H17FN6O2
  • 化合物TAK-063,10 MM DMSO 溶液
  • 化合物TAK-063
  • 化合物 BALIPODECT
  • 1-[2-氟-4-(1H-吡唑-1-基)苯基]-5-甲氧基-3-(1-苯基-1H-吡唑-5-基)哒嗪-4(1H)-酮
  • 1238697-26-1
  • Balipodect, 10 mM in DMSO
  • 4(1H)-Pyridazinone, 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-
  • TAK063, TAK 063, TAK-063, BALIPODECT
  • TAK-063(Balipodect)
  • CS-1534
  • Pyridone 6[1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one]
  • TAK 063;TAK063
  • Balipodect
  • 1-[2-Fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one
  • TAK-063

Home

My