Licostinel
Based on 1 Customer Validation
Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity.
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- Pureté : 98.12%
- CAS No.: 153504-81-5
- Formule: C8H3Cl2N3O4
- Masse moléculaire:276.04
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
59 nM (glycine receptor)[1]
In Vivo
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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.
Chemical Information
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CAS No. 153504-81-5
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Appearance Solid
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Masse moléculaire 276.04
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Formule 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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Synonyms
ACEA-1021
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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 |
Licostinel Related Classifications
HY-117547 Related Classifications
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