MK-0343
Based on 1 Customer Validation
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.
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 : 99.69%
- CAS 番号: 233275-76-8
- 分子式: C19H17F2N7O
- 分子量:397.38
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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
生物活性
製品説明
IC50 & Target
Ki: 0.22 nM (rGABAA α1), 0.4 nM (rGABAAα2) , 0.21 nM (rGABAAα3), 78 nM (rGABAAα4), 0.23 nM (rGABAAα5), 980 nM (rGABAAα6)[1]
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics)[1]
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Dosage:1, 2 or 3 mg/kg
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Administration:Oral administration
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Result:Readily penetrated the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL.
化学情報
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CAS 番号 233275-76-8
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性状 Solid
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分子量 397.38
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分子式 C19H17F2N7O
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Color White to off-white
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SMILES
CN1N=CN=C1COC2=NN3C(C=C2C4CCC4)=NN=C3C5=C(F)C=CC=C5F
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別名
MRK-409
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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
体外:
DMSO : 250 mg/mL (629.12 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 (277 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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取扱説明書 (2659 KB)
参考文献
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 | 2.5165 mL | 12.5824 mL | 25.1648 mL | 62.9121 mL |
| 5 mM | 0.5033 mL | 2.5165 mL | 5.0330 mL | 12.5824 mL | |
| 10 mM | 0.2516 mL | 1.2582 mL | 2.5165 mL | 6.2912 mL | |
| 15 mM | 0.1678 mL | 0.8388 mL | 1.6777 mL | 4.1941 mL | |
| 20 mM | 0.1258 mL | 0.6291 mL | 1.2582 mL | 3.1456 mL | |
| 25 mM | 0.1007 mL | 0.5033 mL | 1.0066 mL | 2.5165 mL | |
| 30 mM | 0.0839 mL | 0.4194 mL | 0.8388 mL | 2.0971 mL | |
| 40 mM | 0.0629 mL | 0.3146 mL | 0.6291 mL | 1.5728 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5033 mL | 1.2582 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4194 mL | 1.0485 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3146 mL | 0.7864 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6291 mL |