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Balipodect

Catalog No. T1745 CAS 1238697-26-1

Synonyms: TAK063, TAK-063, TAK 063

Balipodect (TAK063) is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is <15000-fold over other PDEs.

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Balipodect, CAS 1238697-26-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 94.00
25 mg	In stock	$ 158.00
50 mg	In stock	$ 270.00
100 mg	In stock	$ 468.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 99.28%

Purity: 98.97%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Balipodect (TAK063) is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is >15000-fold over other PDEs.
Targets&IC50	PDE10A:0.3 nM
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 Clinicalal trials for the treatment of schizophrenia[1].
Kinase Assay	Catalytic assay: MEK5 protein isolated from a baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02188. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of an ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value.

Synonyms	TAK063, TAK-063, TAK 063
Molecular Weight	428.42
Formula	C23H17FN6O2
CAS No.	1238697-26-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 79 mg/mL (184.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Kunitomo J, et al. J Med Chem. 2014, 57(22):9627-43.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Lipid Compound Library Clinical Compound Library Bioactive Compound Library Human Metabolite Library Anti-Alzheimer's Disease Compound Library Metabolism Compound Library Orally Active Compound Library

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Keywords

Balipodect 1238697-26-1 Metabolism PDE TAK063 Phosphodiesterase (PDE) inhibit TAK-063 Inhibitor TAK 063 inhibitor

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