Balipodect
Based on 2 publication(s) in Google Scholar
Balipodect (TAK-063) is a selective, brain-penetrant and orally active PDE10A inhibitor with an IC50 of 0.30 nM. Balipodect shows >15000-fold selectivity over other PDEs. Balipodect elevates striatal cAMP and cGMP levels in mice. Balipodect can be used for the study of schizophrenia[1].
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.47%
- CAS. Nr.: 1238697-26-1
- Formel: C23H17FN6O2
- Molecular Weight:428.42
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Balipodect
More
Biologische Aktivität
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PDE10 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1238697-26-1
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Appearance Solid
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Molecular Weight 428.42
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Formel C23H17FN6O2
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Color Light yellow to yellow
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SMILES
FC1=CC(N2N=CC=C2)=CC=C1N3N=C(C4=CC=NN4C5=CC=CC=C5)C(C(OC)=C3)=O
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Synonyms
TAK-063
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Anesthesiology
2025 Feb 1;142(2):332-348. PMID: 39503623 -
Neurobiol Dis
Inhibition of CXCR2 enhances CNS remyelination via modulating PDE10A/cAMP signaling pathway. [Abstract]2023 Feb:177:105988. PMID: 36603746
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (58.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Mice[1]
Compound 27h was suspended in 0.5% (w/v) methylcellulose in distilled water. Compound 27h was administered orally (po). PCP hydrochloride (lot no. 010M4010) purchased from Sigma-Aldrich, Inc. (USA) was dissolved in saline and was administered subcutaneously (sc). All compounds were dosed in a volume of 20 mL/kg body weight. Hyperlocomotion was measured using a spontaneous motor analyzer MDC system (BrainScience idea. Co. Ltd., Japan). Mice were placed in locomotor chambers for more than 60 min for habituation. Animals were removed from each chamber and treated with either vehicle or compound 27h and then quickly returned to the chamber. The following doses were used: 0.1, 0.3, and 1.0 mg/kg, po. Sixty minutes after treatment with compound 27h, animals were again removed from the chambers and treated with either vehicle (saline) or PCP (5 mg/kg as a salt, sc) and then quickly transferred to the test chamber. Activity counts were recorded in successive 1 min bins, and the total number counts were determined for the 120 min period after PCP administration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3342 mL | 11.6708 mL | 23.3416 mL | 58.3539 mL |
| 5 mM | 0.4668 mL | 2.3342 mL | 4.6683 mL | 11.6708 mL | |
| 10 mM | 0.2334 mL | 1.1671 mL | 2.3342 mL | 5.8354 mL | |
| 15 mM | 0.1556 mL | 0.7781 mL | 1.5561 mL | 3.8903 mL | |
| 20 mM | 0.1167 mL | 0.5835 mL | 1.1671 mL | 2.9177 mL | |
| 25 mM | 0.0934 mL | 0.4668 mL | 0.9337 mL | 2.3342 mL | |
| 30 mM | 0.0778 mL | 0.3890 mL | 0.7781 mL | 1.9451 mL | |
| 40 mM | 0.0584 mL | 0.2918 mL | 0.5835 mL | 1.4588 mL | |
| 50 mM | 0.0467 mL | 0.2334 mL | 0.4668 mL | 1.1671 mL |
Balipodect Related Classifications
HY-12472 Related Classifications
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