Licostinel
Based on 1 Customer Validation
Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity.
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 : 98.12%
- CAS 番号: 153504-81-5
- 分子式: C8H3Cl2N3O4
- 分子量:276.04
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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
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生物活性
製品説明
IC50 & Target
59 nM (glycine receptor)[1]
体内実験
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Animal Model:The permanent model of middle cerebral artery occlusion in fisher 344 rats and CD-1 mice.
The transient model of focal ischemia in Wistar and Sprague –Dawley rats [2 -
Dosage:5 mg/kg bolus 3.5 mg/kg/h for 6h, 10 mg/kg bolus 7.0 mg/kg/h for 6h
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Administration:A single intravenous injection bolus continuous infusion
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Result:Decreased infarct size.
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Animal Model:Male Sprague-Dawley rats [3]
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Dosage:20, 40, 80 mg/kg for intraperitoneal injection (i.p.) bolus 7 mg/kg/h , 30mins
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Administration:Intravenous injection (i.v.) bolus continuous infusion
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Result:Reduced the rate of spreading depression and EEG activity in the rat brain in a dose-dependent manner.
化学情報
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CAS 番号 153504-81-5
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性状 Solid
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分子量 276.04
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分子式 C8H3Cl2N3O4
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Color Light yellow to light brown
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SMILES
O=C1NC2=C(NC1=O)C([N+]([O-])=O)=C(C(Cl)=C2)Cl
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別名
ACEA-1021
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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 : 12.5 mg/mL (45.28 mM; ultrasonic and warming and heat to 60°C; 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
[1]. Zhou ZL, et al. Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists. Bioorg Med Chem. 2003 Apr 17;11(8):1769-80. [Content Brief]
[2]. Albers GW, et al. Dose escalation study of the NMDA glycine-site antagonist licostinel in acute ischemic stroke. Stroke. 1999 Mar;30(3):508-13. [Content Brief]
[3]. Martin H, et al. Effects of glycine receptor antagonism on spreading depression in the rat. Neurosci Lett. 1994 Oct 24;180(2):285-9. [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 | 3.6227 mL | 18.1136 mL | 36.2273 mL | 90.5682 mL |
| 5 mM | 0.7245 mL | 3.6227 mL | 7.2455 mL | 18.1136 mL | |
| 10 mM | 0.3623 mL | 1.8114 mL | 3.6227 mL | 9.0568 mL | |
| 15 mM | 0.2415 mL | 1.2076 mL | 2.4152 mL | 6.0379 mL | |
| 20 mM | 0.1811 mL | 0.9057 mL | 1.8114 mL | 4.5284 mL | |
| 25 mM | 0.1449 mL | 0.7245 mL | 1.4491 mL | 3.6227 mL | |
| 30 mM | 0.1208 mL | 0.6038 mL | 1.2076 mL | 3.0189 mL | |
| 40 mM | 0.0906 mL | 0.4528 mL | 0.9057 mL | 2.2642 mL |