Tetrabenazine-d6
Based on 1 Customer Validation
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.
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 : 98.20%
- CAS 番号: 1392826-25-3
- 分子式: C19H21D6NO3
- 分子量:323.46
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
生物活性
製品説明
体外実験
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Potential advantages of deuterated compounds:
(1) Extend the half-life in vivo. Deuterated compounds may be able to prolong the pharmacokinetic characteristics of the compound, that is, prolong the half-life in vivo. This can improve compound safety, efficacy and tolerability, and increase ease of administration.
(2) Improve oral bioavailability. Deuterated compounds may reduce the degree of unwanted metabolism (first-pass metabolism) in the gut wall and liver, allowing a greater proportion of the unmetabolized drug to reach its target site of action. High bioavailability determines its activity at low doses and better tolerance.
(3) Improve metabolic characteristics. Deuterated compounds may reduce the formation of toxic or reactive metabolites and improve drug metabolism.
(4) Improve drug safety. Deuterated compounds may reduce or eliminate adverse side effects of pharmaceutical compounds and are safe.
(5) Preserve the therapeutic properties. Deuterated compounds are expected to retain similar biochemical potency and selectivity to hydrogen analogs in previous studies.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
アプリケーション
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
化学情報
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CAS 番号 1392826-25-3
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非標識Cas 58-46-8
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性状 Solid
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分子量 323.46
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分子式 C19H21D6NO3
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Color Light yellow to yellow
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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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別名
Ro 1-9569-d6
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 33.33 mg/mL (103.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.1 mg/mL (0.31 mM; Need ultrasonic)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (248 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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取扱説明書 (2659 KB)
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 (protect from light). 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 | 3.0916 mL | 15.4579 mL | 30.9157 mL | 77.2893 mL |
| 5 mM | 0.6183 mL | 3.0916 mL | 6.1831 mL | 15.4579 mL | |
| 10 mM | 0.3092 mL | 1.5458 mL | 3.0916 mL | 7.7289 mL | |
| 15 mM | 0.2061 mL | 1.0305 mL | 2.0610 mL | 5.1526 mL | |
| 20 mM | 0.1546 mL | 0.7729 mL | 1.5458 mL | 3.8645 mL | |
| 25 mM | 0.1237 mL | 0.6183 mL | 1.2366 mL | 3.0916 mL | |
| 30 mM | 0.1031 mL | 0.5153 mL | 1.0305 mL | 2.5763 mL | |
| 40 mM | 0.0773 mL | 0.3864 mL | 0.7729 mL | 1.9322 mL | |
| 50 mM | 0.0618 mL | 0.3092 mL | 0.6183 mL | 1.5458 mL | |
| 60 mM | 0.0515 mL | 0.2576 mL | 0.5153 mL | 1.2882 mL | |
| 80 mM | 0.0386 mL | 0.1932 mL | 0.3864 mL | 0.9661 mL | |
| 100 mM | 0.0309 mL | 0.1546 mL | 0.3092 mL | 0.7729 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.