Luvadaxistat
Based on 1 Customer Validation
Luvadaxistat (TAK-831) is an orally active, highly selective, potent D-amino acid oxidase (DAAO) inhibitor. Luvadaxistat inhibits oxidative deamination of D-serine via the human recombinant DAAO enzyme with an IC50 of 14 nM. Luvadaxistat significantly increases D-serine levels in the rodent brain, plasma, and cerebrospinal fluid. Luvadaxistat has the potential for schizophrenia research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.08%
- CAS 番号: 1425511-32-5
- 分子式: C13H11F3N2O2
- 分子量:284.23
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
27 nM
Compound: 28
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Inhibition of human full length DAAO overexpressed in HEK293 cells after 30 mins by plate reader analysis
Inhibition of human full length DAAO overexpressed in HEK293 cells after 30 mins by plate reader analysis
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[PMID: 23566269] |
| HEK293 | IC50 |
5 nM
Compound: 28
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Inhibition of rat full length DAAO overexpressed in HEK293 cells after 30 mins by plate reader analysis
Inhibition of rat full length DAAO overexpressed in HEK293 cells after 30 mins by plate reader analysis
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[PMID: 23566269] |
| HEK293 | IC50 |
5.9 nM
Compound: 28
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Inhibition of mouse full length DAAO overexpressed in HEK293 cells after 30 mins by plate reader analysis
Inhibition of mouse full length DAAO overexpressed in HEK293 cells after 30 mins by plate reader analysis
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[PMID: 23566269] |
Acute dosing of Luvadaxistat (0.3, 1, 3 mg/kg; p.o.) significantly reverses a poly(I:C)-induced deficit social preference in male C57BL/6 poly(I:C)-treated mice[1].
Luvadaxistat (1, 3, 10 mg/kg; p.o. at 2, 6, 10, and 24 h) inhibits DAAO by increased rat cerebellar d-serine levels in a dose- and time-dependent manner with a maximal effect observed at a dose of 10 mg/kg at 10 h post-dose in male Wistar rats weighing 240-280 g[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (aged 9-10 weeks)[1]
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Dosage:0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3 mg/kg
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Administration:PO; daily; 14 days
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Result:Dose-dependently improved social behavior in the SI test in BALB/c animals when dosed chronically (0.01-3 mg/kg).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1425511-32-5
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性状 Solid
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分子量 284.23
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分子式 C13H11F3N2O2
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Color Off-white to light yellow
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SMILES
O=C1C(O)=CC(CCC2=CC=C(C(F)(F)F)C=C2)=NN1
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別名
TAK-831
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 15.62 mg/mL (54.96 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (271 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Rosa Fradley, et al. Luvadaxistat: A Novel Potent and Selective D-Amino Acid Oxidase Inhibitor Improves Cognitive and Social Deficits in Rodent Models for Schizophrenia. [Content Brief]
[2]. Wang H, Norton J, Xu L, DeMartinis N, Sen R, Shah A, Farmer J, Lynch D. Results of a randomized double-blind study evaluating luvadaxistat in adults with Friedreich ataxia. Ann Clin Transl Neurol. 2021 Jun;8(6):1343-1352. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5183 mL | 17.5914 mL | 35.1828 mL | 87.9569 mL |
| 5 mM | 0.7037 mL | 3.5183 mL | 7.0366 mL | 17.5914 mL | |
| 10 mM | 0.3518 mL | 1.7591 mL | 3.5183 mL | 8.7957 mL | |
| 15 mM | 0.2346 mL | 1.1728 mL | 2.3455 mL | 5.8638 mL | |
| 20 mM | 0.1759 mL | 0.8796 mL | 1.7591 mL | 4.3978 mL | |
| 25 mM | 0.1407 mL | 0.7037 mL | 1.4073 mL | 3.5183 mL | |
| 30 mM | 0.1173 mL | 0.5864 mL | 1.1728 mL | 2.9319 mL | |
| 40 mM | 0.0880 mL | 0.4398 mL | 0.8796 mL | 2.1989 mL | |
| 50 mM | 0.0704 mL | 0.3518 mL | 0.7037 mL | 1.7591 mL |
Luvadaxistat 関連分類
HY-109183 関連分類
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