ACT-389949是一种首创、高效、选择性的甲酰肽受体2/脂蛋白A4受体(FPR2)/(ALX)激动剂，对FPR2/ALX进行内化入单核细胞的EC50值为3nM。ACT-389949具有研究炎性疾病的潜力。
货号:ajcx30124
CAS:1258417-54-7
分子式:C20H18F2N6O3
分子量：428.39
溶解度:DMSO: 10 mg/mL (23.34 mM; ultrasonic and adjust pH to 1 with HCl)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

[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.