LY2828360 - Cannabinoid Receptor Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY2828360Cat. No.: HY-16642ACAS No.: 1231220-79-3分式: CHClNO分量: 426.94作靶点: Cannabinoid Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 20.83 mg

2、/mL (48.79 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3422 mL 11.7112 mL 23.4225 mL5 mM 0.4684 mL 2.3422 mL 4.6845 mL10 mM 0.2342 mL 1.1711 mL 2.3422 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现

3、配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.87 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.87 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility:

4、2.08 mg/mL (4.87 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 LY2828360个作缓慢但很有效的 G 蛋偏倚的素受体 2 (CB2) 激动剂，能够抑制 cAMP 的积累并激活 ERK1/2 通路。IC50 & Target CB2 1.体内研究 In WT mice, acute systemic administration of LY2828360 suppresses paclitaxel-induced mechanical and

5、 coldallodynia in a dose-dependent manner. LY2828360 produces time-dependent suppressions of paclitaxel-evoked mechanical and cold hypersensitivities and suppression of allodynia is maintained for at least 4.5 hpost-injection relative to drug pre-injection levels. At 24 h post-injection, paclitaxel-

6、induced mechanicalallodynia has returned to drug pre-injection levels of hypersensitivity. Residual suppression of cold allodyniawas absent by 72 h post LY2828360 treatment. Previously chronic administration of LY2828360 blocks thedevelopment of tolerance to the antiallodynic effects of morphine in

7、WT but not in CB2KO mice. ChronicLY2828360 treatment suppresses paclitaxel-induced mechanical and cold allodynia in WT mice but not inCB2KO mice previously render tolerant to morphine 1.REFERENCES1. Lin X, et al. Slowly Signaling G Protein-Biased CB2 Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain withSustained Efficacy and Attenuates Morphine Tolerance and Dependence. Mol Pharmacol. 2018 Feb;93(2):49-62.McePdfHeightCaution: Product has not been fully validated for medical applications.For rese