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描述 | GPR84 is a medium chain fatty acid (MCFA) receptor, with capric acid (a 10-carbon chain fatty acid) being the most potent ligand. It is highly expressed in the cells of myeloid lineage that constitute the innate immune system, including monocytes, macrophages, and neutrophils in the periphery and microglia in the brain. GPR84 Antagonist 8 is a selective GPR84 antagonist from the patent literature (Galapagos NV Company, US 2013/0165437 A1). As a GPCR antagonist, GPR84 Antagonist 8 dose-dependently inhibited the action of 6-OAU in decreasing cAMP production in GPR84-CHO cells. Blockade of GPR84 activation by pre-treatment with GPR84 Antagonist 8 at 10μM for 30min before adding 1μM GPR84 agonist 6-OAU in LPS pre-treated BMDMs, reduced the expression of TNFα, IL-6, IL12b, CCL2, CCL5, and CXCL1, as well as partially blocked the phosphorylation of AKT and ERK induced by 6-OAU. GPR84 Antagonist 8 at 10μM could antagonize the migration, bacterial adhesion, and phagocytosis promoted by 6-OAU mediated—GPR84 activation in macrophages. Pretreatment with GPR84 Antagonist 8 at 10μM for 1h blocked 6-OAU induced U937 cell migration. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.37mL 0.47mL 0.24mL |
11.86mL 2.37mL 1.19mL |
23.73mL 4.75mL 2.37mL |
CAS号 | 1445846-30-9 |
分子式 | C23H23N3O5 |
分子量 | 421.45 |
SMILES Code | O=C1N=C(OCC2OCCOC2)C=C3N1CCC4=C3C=CC(OCC5=NC=CC=C5)=C4 |
MDL No. | N/A |
别名 | |
运输 | 蓝冰 |
InChI Key | KSGKMLVYIUJQMZ-UHFFFAOYSA-N |
Pubchem ID | 71598639 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 4 mg/mL(9.49 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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