ACT-389949 | FPR2 agonist | Probechem Biochemicals

Chemical Structure : ACT-389949

CAS No.: 1258417-54-7

ACT-389949 (ACT389949)

Catalog No.: PC-62594Not For Human Use, Lab Use Only.

ACT-389949 (ACT389949) is a novel potent and selective formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX) agonist with EC50 of 3 nM for FPR2/ALX internalization into monocytes.

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Biological Activity

ACT-389949 (ACT389949) is a novel potent and selective formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX) agonist with EC50 of 3 nM for FPR2/ALX internalization into monocytes.

ACT-389949 has potential for the treatment of inflammatory disorders.

ACT-389949 is an agonist for FPR2 that triggers functional/signaling repertoires comparable to what has been earlier described for other FPR2 agonists, including neutrophil chemotaxis, granule mobilization and activation of the NADPH-oxidase.

ACT-389949 is as potent as the prototype FPR2 peptide agonist WKYMVM and had the advantage of being resistant to oxidation by MPO-H2O2-halide derived oxidants, as compared to the sensitive WKYMVM.

ACT-389949 include an FPR2-dependent and Gαq-independent transient rise in intracellular Ca2+ and recruitment of β-arrestin in down-stream signals.

ACT-389949 is an excellent tool-compound for further dissection of FPR2-regulated activities in vitro and in vivo.

Physicochemical Properties

M.Wt	428.4
Formula	C20H18F2N6O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Methyl-5-m-tolyl-oxazole-4-carboxylic acid {2-[4-(1,1-difluoro-ethyl)-oxazol-2-ylmethyl]-2H-[1,2,3]triazol-4-yl}-amide

References

1. Stalder AK, et al. Br J Clin Pharmacol. 2017 Mar;83(3):476-486.
2. Lind S, et al. Biochem Pharmacol. 2019 Aug;166:163-173.

ACT-389949 (ACT389949)

Biological Activity

Physicochemical Properties

References

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