LY2828360 - Cannabinoid Receptor Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY2828360Cat. No.: HY-16642ACAS No.: 1231220-79-3分式: CHClNO分量: 426.94作靶點(diǎn): Cannabinoid Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 20.83 mg

2、/mL (48.79 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的?chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)

3、配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.87 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.87 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility:

4、2.08 mg/mL (4.87 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 LY2828360個(gè)作緩慢但很有效的 G 蛋偏倚的素受體 2 (CB2) 激動(dòng)劑，能夠抑制 cAMP 的積累并激活 ERK1/2 通路。IC50 & Target CB2 1.體內(nèi)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