| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Luvadaxistat targets D-amino acid oxidase (DAAO), an enzyme that degrades D-serine, a co-agonist of NMDA receptors. By inhibiting DAAO, Luvadaxistat increases D-serine levels, which enhances NMDA receptor functionality. This mechanism is being explored for the treatment of schizophrenia and other neurological conditions.
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| ln Vitro |
In vitro, Luvadaxistat inhibits human recombinant DAAO with an IC50 of 14 nM. It is a highly selective and potent inhibitor. The compound significantly increases D-serine levels in rodent brains.
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| ln Vivo |
In vivo, Luvadaxistat significantly increases D-serine levels in the brains of rodents. It is being investigated in clinical trials for the treatment of schizophrenia and Friedreich's ataxia. The compound is under investigation in clinical trial NCT03214588.
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| Enzyme Assay |
The in vitro enzyme assay for Luvadaxistat involves measuring the inhibition of DAAO enzymatic activity. Recombinant human DAAO is incubated with D-serine in the presence of varying concentrations of the compound. The production of the oxidative deamination product is measured, and the IC50 of 14 nM is determined.
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| Cell Assay |
Cellular assays for Luvadaxistat are performed using cells expressing DAAO. Cells are treated with the compound at various concentrations. D-serine levels are measured in the cell culture medium. The compound's ability to inhibit DAAO and increase D-serine levels is assessed.
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| Animal Protocol |
In vivo animal studies for Luvadaxistat are conducted in rodents. The compound is administered orally. D-serine levels in the brain are measured to assess target engagement. Behavioral tests are performed to evaluate the compound's effects on cognitive function.
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| ADME/Pharmacokinetics |
Luvadaxistat is an orally active compound with favorable pharmacokinetic properties. It is being developed as a therapeutic agent for central nervous system indications. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for Luvadaxistat are not reported in the available sources. As an investigational compound, it has been evaluated in preclinical models and clinical trials. Specific toxicological profiles are not provided in the supplier documentation.
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| References |
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| Additional Infomation |
Luvadaxistat is being investigated in the clinical trial NCT03214588 (Efficacy, tolerability and pharmacokinetics of multiple oral doses of TAK-831 in adult Friedreich ataxia).
Luvadaxistat is an investigational drug being developed for the treatment of schizophrenia and Friedreich's ataxia. It is a potent and selective DAAO inhibitor that increases D-serine levels and enhances NMDA receptor function. The compound is available from commercial suppliers for research purposes. |
| Molecular Formula |
C13H11F3N2O2
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|---|---|
| Molecular Weight |
284.2339
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| Exact Mass |
284.077
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| CAS # |
1425511-32-5
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| PubChem CID |
71270546
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.557
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| LogP |
1.76
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
424
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])C1=C([H])C(C(N([H])N1[H])=O)=O)(F)F
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| InChi Key |
QBQMUMMSYHUDFM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H11F3N2O2/c14-13(15,16)9-4-1-8(2-5-9)3-6-10-7-11(19)12(20)18-17-10/h1-2,4-5,7H,3,6H2,(H,17,19)(H,18,20)
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| Chemical Name |
6-[2-[4-(trifluoromethyl)phenyl]ethyl]-1,2-dihydropyridazine-3,4-dione
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| Synonyms |
Luvadaxistat; TAK-831; TAK831; TAK 831; Luvadaxistat [USAN]; 76IC00YRVR; UNII-76IC00YRVR;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~16.67 mg/mL (~58.65 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5183 mL | 17.5914 mL | 35.1828 mL | |
| 5 mM | 0.7037 mL | 3.5183 mL | 7.0366 mL | |
| 10 mM | 0.3518 mL | 1.7591 mL | 3.5183 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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