| Identification | Back Directory | [Name]
ACT-389949
(ACT389949) | [CAS]
1258417-54-7 | [Synonyms]
ACT-389949
(ACT389949)
2-methyl-5-m-tolyloxazol-4-carboxylic acid {2-[4-(1,1-difluoroethyl)-oxazol-2-ylmethyl]-2H-[1,2,3]triazol-4-yl}amide
N-[2-[[4-(1,1-difluoroethyl)-1,3-oxazol-2-yl]methyl]triazol-4-yl]-2-methyl-5-(3-methylphenyl)-1,3-oxazole-4-carboxamide
4-Oxazolecarboxamide, N-[2-[[4-(1,1-difluoroethyl)-2-oxazolyl]methyl]-2H-1,2,3-triazol-4-yl]-2-methyl-5-(3-methylphenyl)- | [Molecular Formula]
C20H18F2N6O3 | [MDL Number]
MFCD32708507 | [MOL File]
1258417-54-7.mol | [Molecular Weight]
428.39 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. DOI:10.1111/bcp.13149
[2] Lind S, et al. Functional and signaling characterization of the neutrophil FPR2 selective agonist Act-389949. Biochem Pharmacol. 2019 Aug;166:163-173. DOI:10.1016/j.bcp.2019.04.030 |
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