| Size | Price | Stock | Qty |
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| 500μg |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Deutetrabenazine (formerly known as SD-809; GTPL8707; tetrabenazine-d6; trade name Austedo), the hexa-deuterated form of tetrabenazine, is an orally bioactive, small-molecule vesicular monoamine transporter 2 (VMAT2) inhibitor which has been approved by FDA in 2017 for the treatment of chorea associated with Huntington's disease and tardive dyskinesia. Chemically, deutetrabenazine is an isotopic/deuterated isomer of tetrabenazine in which six hydrogen atoms have been replaced by deuterium atoms. The incorporation of deuterium slows the rate of drug metabolism, allowing less frequent dosing. Teva Pharmaceuticals received approvals from the Food and Drug Administration to market deutetrabenazine in early 2017, along with five years of orphan drug exclusivity for the treatment of chorea associated with Huntington's Disease. At the time, it was the only deuterated drug to have received FDA approval.
| ln Vitro |
Drug compounds have been modified to include stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers that influence quantification during the drug development process. It's possible that the pharmacokinetics and functional range of medications contribute to the concern of mutagenesis. [1]. Possible benefits of compounds with delayed generation: (1) One possible benefit of delayed-generation compounds is that they may be able to extend the compound's pharmacokinetic properties. Potential benefits of compounds with delayed generation: (1) Compounds with delayed generation could be It can extend a compound's pharmacokinetic properties, extending its safety, tolerability, and ability to withstand adverse reactions in delayed-generation drugs. Enhance intestinal absorption. Deuterated compounds have the potential to decrease the level of first-pass metabolism required in the intestinal wall and colon, which would enable a higher percentage of the medicine to remain unmetabolized and achieve high bioavailability levels. These levels define the drug's efficacy at low dosages and improve its tolerability. Enhance the properties of metabolism. medication safety, medication metabolism, and toxic or reactive metabolite reduction are all potential benefits of metabolites (4). Deuterated chemicals are harmless and have the potential to lessen or eliminate the negative effects of medicinal compounds. (5) Preserve their medicinal qualities. According to earlier research, deuterated chemicals ought to maintain comparable effects and biochemical efficacy to their hydrogen counterparts.
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| References |
The Lancet. 2017,4(8): 595–604.
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| Molecular Formula |
C19H21D6NO3
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| Molecular Weight |
323.47
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| CAS # |
1392826-25-3
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| Related CAS # |
Tetrabenazine;58-46-8;Tetrabenazine Racemate;718635-93-9;(+)-Tetrabenazine;1026016-83-0;(+)-Tetrabenazine-d6;1977511-05-9
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| SMILES |
O=C1[C@H](CC(C)C)CN2CCC3=CC(OC([2H])([2H])[2H])=C(OC([2H])([2H])[2H])C=C3[C@@]2([H])C1
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| Chemical Name |
rel-(3R,11bR)-3-isobutyl-9,10-bis(methoxy-d3)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one
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| Synonyms |
Deutetrabenazine; Tetrabenazine-d6; SD809; GTPL-8707; SD-809; GTPL8707; SD 809; GTPL 8707; trade name Austedo
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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) |
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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 | 3.0915 mL | 15.4574 mL | 30.9148 mL | |
| 5 mM | 0.6183 mL | 3.0915 mL | 6.1830 mL | |
| 10 mM | 0.3091 mL | 1.5457 mL | 3.0915 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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