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.
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: 99.35%
- CAS 番号: 2250025-91-1
- 分子式: C23H26ClFN4O4S
- 分子量:508.99
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保管条件:
-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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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.
化学情報
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CAS 番号 2250025-91-1
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性状 Solid
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分子量 508.99
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
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.
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 (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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取扱説明書 (2659 KB)
参考文献
[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 |
LEI-101 関連分類
HY-124283A 関連分類
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