ACT-389949
产品说明书
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同义名 : | - |
| CAS号 : | 1258417-54-7 | |
| 货号 : | A1339031 | |
| 分子式 : | C20H18F2N6O3 | |
| 纯度 : | 98%+ | |
| 分子量 : | 428.39 | |
| MDL号 : | MFCD32263022 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The formyl peptide receptors (FPRs), belonging to the family of G-protein coupled receptors (GPCRs), predominantly govern a proinflammatory response resulting in chemotaxis, degranulation, and oxidative burst during infection. ACT-389949 is a new potent (EC50 3 nM = 1.3 ng/mL for FPR2 internalisation on monocytes) and selective FPR2 agonist that holds potential for the treatment of inflammatory disorders[2]. In human neutrophils, ACT-389949 induced a transient rise in [Ca2+]i with a concentration in the low nM range. Similar to the FPR2 peptide agonist WKYMVM, ACT-389949 triggered β-arrestin 2 recruitment in cells expressing FPR2[3]. Administration of ACT-389949 in healthy subjects resulted in a dose-dependent, long-lasting internalisation of FPR2 leukocytes. Pro- and anti-inflammatory cytokines were dose-dependently and transiently up-regulated after the first dose[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.33mL 0.47mL 0.23mL |
11.67mL 2.33mL 1.17mL |
23.34mL 4.67mL 2.33mL |
| 参考文献 |
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