| Description | ACT-389949 is a potent and selective agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. It has the potential for the treatment of inflammatory disorders. |
| In vivo | ACT-389949在体内得到良好耐受。该化合物在给药后约2小时达到最大浓度,平均终末半衰期为29.3小时。ACT-389949的给药可引起剂量依赖性,长效的FPR2/ALX在白细胞内的内化作用[1]。 |
| Target activity | FPR2/ALX:3 nM(EC50) |
| molecular weight | 428.39 |
| Molecular formula | C20H18F2N6O3 |
| CAS | 1258417-54-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 10 mg/mL (23.34 mM), when pH is adjusted to 1 with HCl. Sonication is recommended. |
| 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. |