LEI 101 hydrochloride

Pricing Availability   Qty
说明: Potent and selective CB2 partial agonist; orally biovailable
化学名: 3-Cyclopropyl-1-[[4-[6-[(1,1-dioxido-4-thiomorpholinyl)methyl]-5-fluoro-2-pyridinyl]phenyl]methyl]-2,4-imidazolidinedione hydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (1)

生物活性 for LEI 101 hydrochloride

LEI 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.

技术数据 for LEI 101 hydrochloride

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.

溶解性数据 for LEI 101 hydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 50.9 100

制备储备液 for LEI 101 hydrochloride

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for LEI 101 hydrochloride

参考文献 for LEI 101 hydrochloride

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


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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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Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.