GPR84-antagonist-8 - GPR84 Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGPR84 antagonist 8Cat. No.: HY-112562CAS No.: 1445846-30-9分式: CHNO分量: 421.45作靶点: GPR84作通路: GPCR/G Protein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 : 5 mg/mL (11.86 mM; Need ultrasonic)M

2、ass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3728 mL 11.8638 mL 23.7276 mL5 mM 0.4746 mL 2.3728 mL 4.7455 mL10 mM 0.2373 mL 1.1864 mL 2.3728 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，配制前请先配制澄清的储备液，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，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前

3、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: 0.54 mg/mL (1.28 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.54 mg/mL (1.28 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.54 mg/mL (1.28 mM); Clear so

4、lution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 GPR84 antagonist 8种选择性 GPR84 拮抗剂。IC50 & Target GPR84 1体外研究 GPR84 is a member of the metabolic G protein-coupled receptor family, and its expression has beendescribed predominantly in immune cells. To test the hypothesis th

5、at blocking the activation of GPR84 canbe a potential anti-inflammatory strategy in different inflammatory diseases, GPR84 antagonist 8 is used. Thepotency and specificity of GPR84 antagonist 8 is assessed tusing GPR84-CHO cells in the cAMP assay.GPR84 antagonist 8 effectively inhibits the action of

6、 6-OAU in decreasing cAMP production in GPR84-CHOcells. To test GPR84 antagonist 8s inhibition of the pro-inflammatory effects of GPR84 activation inmacrophages, LPS pre-treated BMDMs are incubated with 10M GPR84 antagonist 8 for 30min beforeadding 1M 6-OAU. Protein analysis by Western Blot shows th

7、at the GPR84 antagonist 8 partially blocks thephosphorylation of AKT and ERK induced by 6-OAU 1.PROTOCOLCell Assay 1 Bone marrow-derived macrophages treated with either vehicle (0.3% DMSO) or 1M 6-OAU for 1h areincubated with unopsonised pHrodo E. coli bioparticles at 0.1mg/mL in a 96-well flat clea

8、r bottom plate. Forthe inhibition studies with GPR84 antagonist 8, cells are pretreated with 10M GPR84 antagonist 8 for 30min before addition of either vehicle or 6-OAU. The plate is then placed into the IncuCyte Zoom platformwhich is housed inside a humidified incubator at 37C, 5% CO2. Two to four

9、images per well from threetechnical replicates are taken every 15min for 4h 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Recio C, et al. Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages. FrontImmunol. 2018 Jun 20;9:1419.McePdfHeightCaution: Product has not been fully validated for med