产品说明书

ACT-389949

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Chemical Structure| 1258417-54-7 同义名 : -
CAS号 : 1258417-54-7
货号 : A1339031
分子式 : C20H18F2N6O3
纯度 : 98%+
分子量 : 428.392
MDL号 : MFCD32263022
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 9 mg/mL(21.01 mM),配合低频超声,并调节pH至1,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 The formyl peptide receptors (FPRs), belonging to the family of G-protein coupled receptors (GPCRs), predominantly govern a proinflammatory response resulting in chemotaxis, degranulation, and oxidative burst during infection. ACT-389949 is a new potent (EC50 3 nM = 1.3 ng/mL for FPR2 internalisation on monocytes) and selective FPR2 agonist that holds potential for the treatment of inflammatory disorders[2]. In human neutrophils, ACT-389949 induced a transient rise in [Ca2+]i with a concentration in the low nM range. Similar to the FPR2 peptide agonist WKYMVM, ACT-389949 triggered β-arrestin 2 recruitment in cells expressing FPR2[3]. Administration of ACT-389949 in healthy subjects resulted in a dose-dependent, long-lasting internalisation of FPR2 leukocytes. Pro- and anti-inflammatory cytokines were dose-dependently and transiently up-regulated after the first dose[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.67mL

2.33mL

1.17mL

23.34mL

4.67mL

2.33mL

参考文献

[1]Stalder AK, Lott D, Strasser DS, et al. Biomarker-guided clinical development of the first-in-class anti-inflammatory FPR2/ALX agonist ACT-389949. Br J Clin Pharmacol. 2017;83(3):476-486.

[2]Stalder AK, Lott D, 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.

[3]Lind S, Sundqvist M, et al. Functional and signaling characterization of the neutrophil FPR2 selective agonist Act-389949. Biochem Pharmacol. 2019 Aug;166:163-173