Cas No.: | 1258417-54-7 |
Chemical Name: | 2-Methyl-5-m-tolyl-oxazole-4-carboxylic acid {2-[4-(1,1-difluoro-ethyl)-oxazol-2-ylmethyl]-2H-[1,2,3]triazol-4-yl}-amide |
Synonyms: | ACT389949,ACT 389949,ACT-389949 |
SMILES: | O=C(C1=C(C2=CC=CC(C)=C2)OC(C)=N1)NC3=NN(CC4=NC(C(F)(F)C)=CO4)N=C3 |
Formula: | C20H18F2N6O3 |
M.Wt: | 428.4 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
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]. |
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. |