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 EC 50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders.
性状
Solid
IC50 & Target[1][2]
(FPR2)/(ALX)
体内研究(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.
Administration of ACT-389949 results in a dose-dependent, long-lasting internalization of FPR2/ALX into leukocytes. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years该产品在溶液状态不稳定,建议您现用现配,即刻使用。
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 10 mg/mL (23.34 mM; ultrasonic and adjust pH to 1 with HCl)配制储备液