|N-(2-((4-(1,1-二氟乙基)恶唑-2-基)甲基)-2H-1,2,3-三唑-4-基)-2-甲基-5-(间甲苯基)恶唑-4-甲酰胺|CsnPharm

CAS No.: 1258417-54-7

ACT-389949 is a potent and selective agonist of formyl peptide receptor type 2 (FPR2).

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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].
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