| Name | Balipodect |
| Description | Balipodect (TAK063) is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is >15000-fold over other PDEs. |
| 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. |
| 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]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 79 mg/mL (184.4 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.67 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Phosphodiesterase (PDE) | phosphodiesterase | PDE10A | Inhibitor | inhibit | Balipodect |
| Inhibitors Related | Theophylline monohydrate | Acefylline | D(+)-Raffinose pentahydrate | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline | Sildenafil citrate |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Metabolism Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
