LEI-101
Based on 1 Customer Validation
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.35%
- No. CAS: 2250025-91-1
- Fòrmula: C23H26ClFN4O4S
- Peso molecular:508.99
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
LEI-101 (p.o. or i.p.) at 3 or 10 mg/kg dose-dependently prevents kidney dysfunction and/or morphological damage induced by cisplatin in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Neuropathy-induced mechanical allodynia in male wistar rats[1].
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Dosage:2, 6, and 20 mg/kg.
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Administration:PO, single dose.
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Result:Induced a dose-dependent antinociceptive effect after 2 h of dosing.
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Animal Model:Fed male Wistar rats[1].
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Dosage:1 mg/kg iv and 5 mg/kg po (Pharmacological Analysis).
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Administration:IV and PO.
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Result:Exhibited T1/2 of 1.7 h and 0.8 h for po and iv administration.
Had a low clearance and 100% oral bioavailability.
Chemical Information
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No. CAS 2250025-91-1
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Appearance Solid
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Peso molecular 508.99
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Fòrmula C23H26ClFN4O4S
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Color White to off-white
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SMILES
O=C1N(C2CC2)C(CN1CC3=CC=C(C4=NC(CN5CCS(CC5)(=O)=O)=C(F)C=C4)C=C3)=O.[H]Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 116.67 mg/mL (229.22 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mario van der Stelt, et al. Discovery and Optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione Derivatives as a Novel Class of Selective Cannabinoid CB2 Receptor Agonists. J Med Chem. 2011 Oct 27;54(20):7350-62. [Content Brief]
[2]. Partha Mukhopadhyay, et al. The Novel, Orally Available and Peripherally Restricted Selective Cannabinoid CB2 Receptor Agonist LEI-101 Prevents Cisplatin-Induced Nephrotoxicity. Br J Pharmacol. 2016 Feb;173(3):446-58. [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 (sealed storage, away from moisture). 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 | 1.9647 mL | 9.8234 mL | 19.6468 mL | 49.1169 mL |
| 5 mM | 0.3929 mL | 1.9647 mL | 3.9294 mL | 9.8234 mL | |
| 10 mM | 0.1965 mL | 0.9823 mL | 1.9647 mL | 4.9117 mL | |
| 15 mM | 0.1310 mL | 0.6549 mL | 1.3098 mL | 3.2745 mL | |
| 20 mM | 0.0982 mL | 0.4912 mL | 0.9823 mL | 2.4558 mL | |
| 25 mM | 0.0786 mL | 0.3929 mL | 0.7859 mL | 1.9647 mL | |
| 30 mM | 0.0655 mL | 0.3274 mL | 0.6549 mL | 1.6372 mL | |
| 40 mM | 0.0491 mL | 0.2456 mL | 0.4912 mL | 1.2279 mL | |
| 50 mM | 0.0393 mL | 0.1965 mL | 0.3929 mL | 0.9823 mL | |
| 60 mM | 0.0327 mL | 0.1637 mL | 0.3274 mL | 0.8186 mL | |
| 80 mM | 0.0246 mL | 0.1228 mL | 0.2456 mL | 0.6140 mL | |
| 100 mM | 0.0196 mL | 0.0982 mL | 0.1965 mL | 0.4912 mL |
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