产品说明书
GPR84 antagonist 8
 |
同义名 : | - |
| CAS号 : | 1445846-30-9 | |
| 货号 : | A213199 | |
| 分子式 : | C23H23N3O5 | |
| 纯度 : | 97% | |
| 分子量 : | 421.446 | |
| MDL号 : | N/A | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
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 |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 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. | ||
| 实验方案 | |||
|---|---|---|---|
| 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 |
