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Submit ReviewLEI 101 hydrochloride is a potent and selective CB2 partial agonist (pEC50 = 8.0). Exhibits >100-fold selectivity for CB2 over CB1 and no significant interaction with hFAAH, MAGL, DAGL or NAPE-PLD. Displays antinociceptive activity in a rat neuropathic pain model and attenuates renal inflammation in a mouse kidney damage model. Orally bioavailable with low brain penetration.
分子量 | 508.99 |
公式 | C23H25FN4O4S.HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2250025-91-1 |
PubChem ID | 127021038 |
InChI Key | APLLNJWPLUIBCG-UHFFFAOYSA-N |
Smiles | FC1=CC=C(C2=CC=C(C=C2)CN3CC(N(C3=O)C4CC4)=O)N=C1CN5CCS(=O)(CC5)=O.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 50.9 | 100 |
以下数据基于产品分子量 508.99。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.96 mL | 9.82 mL | 19.65 mL |
5 mM | 0.39 mL | 1.96 mL | 3.93 mL |
10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
参考文献是支持产品生物活性的出版物。
van der Stelt M et al (2011) 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. 54 7350 PMID: 21923175
Mukhopadhyay et al (2016) The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity. Br.J.Pharmacol. 173 446 PMID: 26398481
If you know of a relevant reference for LEI 101 hydrochloride, please let us know.
关键词: LEI 101 hydrochloride, LEI 101 hydrochloride supplier, LEI101, hydrochloride, cannabinoid, CB2, partial, agonists, potent, selective, agonism, orally, bioavailable, anti-inflammatory, Receptors, 5826, Tocris Bioscience
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