|2-((1,4-二氧六环-2-基)甲氧基)-9-(吡啶-2-基甲氧基)-6,7-二氢-4H-嘧啶并[6,1-a]异喹啉-4-酮|CsnPharm

CAS No.: 1445846-30-9

GPR84 antagonist 8 Catalog No. CSN22421

Synonyms: GPR84 Antagonist 8

GPR84 antagonist 8 is a selective GPR84 antagonist.

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靶点选择性

生物活性

实验方案

技术信息

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

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3728 mL
- 11.8639 mL
- 23.7278 mL
- 5 mM
- 0.4746 mL
- 2.3728 mL
- 4.7456 mL
- 10 mM
- 0.2373 mL
- 1.1864 mL
- 2.3728 mL

技术信息

CAS号

1445846-30-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H23N3O5

运输

蓝冰

分子量

421.45

别名

GPR84 Antagonist 8

溶解度

DMSO	5.0 mg/mL (11.9 mM) warming

动物实验配方

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