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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-LY2828360
LY2828360

Chemical Structure : LY2828360

CAS No.: 1231220-79-3

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LY2828360 (LY 2828360)

货号: PC-47097Not For Human Use, Lab Use Only.

LY2828360 is a potent CB2 receptor agonist with similar affinity for human and rat CB2 receptors with Ki of 40.3 nM and 36.7 nM, respectively, shows EC50 of 20.1 nM in [35S]-GTPγS assays.

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10 mg ￥880 In stock
25 mg ￥1480 In stock
50 mg ￥2480 In stock
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

LY2828360 is a potent CB2 receptor agonist with similar affinity for human and rat CB2 receptors with Ki of 40.3 nM and 36.7 nM, respectively, shows EC50 of 20.1 nM in [35S]-GTPγS assays.
LY2828360 displays no agonist activity for CB1 receptor (EC50>10 uM).
LY2828360 is a slowly acting but efficacious G protein–biased CB2 agonist, inhibiting cAMP accumulation and activating extracellular signal-regulated kinase 1/2 signaling while failing to recruit arrestin, activate inositol phosphate signaling, or internalize CB2 receptors.
LY2828360 shows good CNS penetration and potent oral activity in a preclinical model of joint pain induced by intra-articular monoiodoacetic acid.
LY2828360 (0.3 mg/kg p.o.) produces a dose-related reversal of pain using incapacitance testing, demonstrating equivalent efficacy to the nonsteroidal anti-inflammatory drug diclofenac in the monoiodoacetic acid model.

物理化学性质&存储条件

分子量 426.949
分子式 C22H27ClN6O
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

8-(2-chlorophenyl)-2-methyl-6-(4-methylpiperazin-1-yl)-9-(tetrahydro-2H-pyran-4-yl)-9H-purine

参考文献

1. Lin X, et al. Mol Pharmacol. 2018 Feb;93(2):49-62.

2. Iyer V, et al. Eur J Pharmacol. 2020 Nov 5;886:173544.

3. Hollinshead SP, J Med Chem 56:5722–5733.

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