Bioactivity | 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) | |||
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]. | |||
Name | ACT-389949 | |||
CAS | 1258417-54-7 | |||
Formula | C20H18F2N6O3 | |||
Molar Mass | 428.39 | |||
Appearance | Solid | |||
Transport | Room temperature in continental US; may vary elsewhere. | |||
Storage |
*该产品在溶液状态不稳定,建议您现用现配,即刻使用。 |
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Reference | [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. |