Home Metabolism PDE inhibitor TAK-063 For research use only.

TAK-063

Synonyms: Balipodect

TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.

TAK-063 Chemical Structure

TAK-063 Chemical Structure

CAS: 1238697-26-1

Selleck's TAK-063 has been cited by 1 publication

Purity & Quality Control

Batch: S845901 DMSO] 85 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.11%
99.11

TAK-063 Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

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Biological Activity

Description TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.
Targets
PDE10A [1]
(Cell-free assay)
0.3 nM
In Vivo
In vivo TAK-063 has high brain penetration in mice. Oral administration of TAK-063 to mice elevated striatal cAMP and (cGMP) levels at 0.3 mg/kg and shows potent suppression of phencyclidine (PCP)-induced hyperlocomotion at a minimum effective dose (MED) of 0.3 mg/kg. TAK-063 is currently being evaluated in clinical trials for the treatment of schizophrenia[1].
Animal Research Animal Models ICR mice
Dosages 0.3 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02370602 Completed
Healthy Volunteers
Takeda
 October 2013 Phase 1
NCT01892189 Completed
Ketamine-Induced Brain Activity Changes|Psychotic-like Symptoms
Takeda
 August 2013 Phase 1
NCT01879722 Completed
Schizophrenia
Takeda
 June 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 428.42 Formula

C23H17FN6O2
CAS No. 1238697-26-1 SDF Download TAK-063 SDF
Smiles COC1=CN(N=C(C1=O)C2=CC=NN2C3=CC=CC=C3)C4=C(C=C(C=C4)N5C=CC=N5)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 85 mg/mL ( (198.4 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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