1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

TAK-063 

Cat. No.: HY-12472 Purity: 98.90%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
TAK-063 Chemical Structure

TAK-063 Chemical Structure

CAS No. : 1238697-26-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
5 mg $70 In-stock
10 mg $90 In-stock
50 mg $250 In-stock
100 mg $440 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs. IC50 value: 0.3 nM [1] Target: PDE10A inhibitor TAK-063 has potent inhibitory activity (IC50 = 0.30 nM), excellent selectivity (>15000-fold selectivity over other PDEs), and favorable pharmacokinetics, including high brain penetration, in mice. Oral administration of 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]. 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. 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. TAK-063 did not affect plasma prolactin or glucose levels at doses up to 3 mg/kg, p.o. TAK-063 at 3 mg/kg, p.o., elicited a weak cataleptic response compared with haloperidol and olanzapine [2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02370602 Takeda Healthy Volunteers October 2013 Phase 1
NCT02477020 Takeda Schizophrenia July 2015 Phase 2
NCT01892189 Takeda Ketamine-Induced Brain Activity Changes|Psychotic-like Symptoms August 2013 Phase 1
NCT01879722 Takeda Schizophrenia June 2013 Phase 1
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References
Molecular Weight

428.42

Formula

C₂₃H₁₇FN₆O₂

CAS No.

1238697-26-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
TAK-063
Cat. No.:
HY-12472
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