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ACT-389949

Names

[ CAS No. ]:
1258417-54-7

[ Name ]:
ACT-389949

Biological Activity

[Description]:

ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others

[Target]

(FPR2)/(ALX)[1]


[In Vivo]

ACT-389949 has well tolerated. Maximum concentrations are reached around 2 hours after dosing, with a mean terminal half-life of 29.3 hours[1]. Administration of ACT-389949 results in a dose-dependent, long-lasting internalization of FPR2/ALX into leukocytes[1].

[References]

[1]. Stalder AK,et al. Biomarker-guided clinical development of the first-in-class anti-inflammatory FPR2/ALX agonist ACT-389949. Br J Clin Pharmacol. 2017 Mar;83(3):476-486.

[2]. Lind S, et al. Functional and signaling characterization of the neutrophil FPR2 selective agonist Act-389949. Biochem Pharmacol. 2019 Aug;166:163-173.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H18F2N6O3

[ Molecular Weight ]:
428.39

Related Compounds