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TAK-063

Product Name
TAK-063
CAS No.
1238697-26-1
Chemical Name
TAK-063
Synonyms
CS-1534;TAK-063;Balipodect;TAK-063 ，S8459;TAK 063;TAK063;TAK-063(Balipodect);Balipodect, 10 mM in DMSO;TAK063, TAK 063, TAK-063, BALIPODECT;1-[2-Fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one;4(1H)-Pyridazinone, 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-
CBNumber
CB62735539
Molecular Formula
C23H17FN6O2
Formula Weight
428.42
MOL File
1238697-26-1.mol
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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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
22208
Product name
TAK-063
Purity
≥98%
Packaging
5mg
Price
$86
Updated
2024/03/01
Cayman Chemical
Product number
22208
Product name
TAK-063
Purity
≥98%
Packaging
10mg
Price
$135
Updated
2024/03/01
Cayman Chemical
Product number
22208
Product name
TAK-063
Purity
≥98%
Packaging
25mg
Price
$212
Updated
2024/03/01
Cayman Chemical
Product number
22208
Product name
TAK-063
Purity
≥98%
Packaging
50mg
Price
$336
Updated
2024/03/01
ChemScene
Product number
CS-3551
Product name
Balipodect
Purity
98.69%
Packaging
5mg
Price
$84
Updated
2021/12/16
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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

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TAK-063 Suppliers

China 93 The Netherlands 1 United States 8 Global 102
Axon Medchem BV
Tel
--
Fax
--
Email
info@axonmedchem.com
Country
The Netherlands
ProdList
477
Advantage
30
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View Lastest Price from TAK-063 manufacturers

Career Henan Chemical Co
Product
Pyridone 6[1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one] 1238697-26-1
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2019-12-30

1238697-26-1, TAK-063Related Search:

RESATORVID TAK-960 TAK-733 Vonoprazan fumarate INK1117

  • 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
  • 4(1H)-Pyridazinone, 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-
  • Balipodect, 10 mM in DMSO
  • TAK-063 ，S8459
  • 1- [2-Fluoro-4- (1H-pyrazol-1-yl) phenyl] -5-methoxy-3- (1-phenyl-1H-pyrazol-5-yl) pyridazine-4 (1H) - one
  • 1238697-26-1
  • C23H17FN6O2
  • Inhibitors