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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-LEI-101 free base
LEI-101 free base

Chemical Structure : LEI-101 free base

CAS No.: 1228660-00-1

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LEI-101 free base (LEI101, LEI 101)

货号: PC-20747Not For Human Use, Lab Use Only.

LEI-101 free base (LEI 101) is a potent, selective, orally available and peripherally restricted cannabinoid CB2 receptor agonist with binding pKi of 7.5 (hCB2R).

规格 价格 库存 数量
5 mg ￥1480 In stock
10 mg ￥2180 In stock
25 mg ￥3580 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LEI-101 free base (LEI 101) is a potent, selective, orally available and peripherally restricted cannabinoid CB2 receptor agonist with binding pKi of 7.5 (hCB2R).
LEI-101 displays 100-fold selectivity for CB2 receptors over CB1 receptors in binding assays, does not interact with other proteins of the endocannabinoid system: human FAAH (hFAAH), MAGL, NAPE-PLD and DAGL.
LEI-101 behaves as a CB2 receptor partial agonist in the β-arrestin recruitment and GTPγS assays with pEC50 of 8.0 and 7.0, respectively.
LEI-101 (60 mg/kg, p.o.) does not induce cannabimimetic effects in vivo.
LEI-101 (3.0 or 10 mg/kg, p.o. and i.p.) attenuates biomarkers and histological damage of cisplatin-induced nephropathy in C57Bl6/J mice, prevents cisplatin-induced increases in serum creatinine and BUN levels.
LEI-101 attenuates cisplatin-induced renal 3-nitrotyrosine (3-NT) formation, attenuates cisplatin (Cis)-induced renal HNE adducts formation in wild type, but not in CB2R-/- mice.

物理化学性质&存储条件

分子量 472.54
分子式 C23H25FN4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-cyclopropyl-1-(4-(6-((1,1-dioxidothiomorpholino)methyl)-5-fluoropyridin-2-yl)benzyl)imidazolidine-2,4-dione

参考文献

1. Mukhopadhyay P, et al. Br J Pharmacol. 2016 Feb;173(3):446-58.

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