ACT-389949 | CAS#1258417-54-7 | FPR2\ALX agonist

MedKoo Cat#: 462068 | Name: ACT-389949

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

ACT-389949

CAS#1258417-54-7

Theoretical Analysis

MedKoo Cat#: 462068

Name: ACT-389949

CAS#: 1258417-54-7

Chemical Formula: C20H18F2N6O3

Exact Mass: 428.1408

Molecular Weight: 428.40

Elemental Analysis: C, 56.07; H, 4.24; F, 8.87; N, 19.62; O, 11.20

Price and Availability

Size	Price	Availability
25mg	USD 850.00	2 Weeks
50mg	USD 1,350.00	2 Weeks
100mg	USD 1,850.00	2 Weeks
200mg	USD 2,650.00	2 Weeks
500mg	USD 3,950.00	2 Weeks
1g	USD 4,950.00	2 Weeks
2g	USD 7,950.00	2 Weeks

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Related CAS #

No Data

Synonym

ACT-389949; ACT389949; ACT 389949

IUPAC/Chemical Name

N-(2-((4-(1,1-difluoroethyl)oxazol-2-yl)methyl)-2H-1,2,3-triazol-4-yl)-2-methyl-5-(m-tolyl)oxazole-4-carboxamide

InChi Key

PBTWPEDVIMHJEO-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H18F2N6O3/c1-11-5-4-6-13(7-11)18-17(24-12(2)31-18)19(29)26-15-8-23-28(27-15)9-16-25-14(10-30-16)20(3,21)22/h4-8,10H,9H2,1-3H3,(H,26,27,29)

SMILES Code

O=C(NC1=NN(N=C1)CC2=NC(C(F)(C)F)=CO2)C3=C(OC(C)=N3)C4=CC=CC(C)=C4

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 428.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Lind S, Sundqvist M, Holmdahl R, Dahlgren C, Forsman H, Olofsson P. Functional and signaling characterization of the neutrophil FPR2 selective agonist Act-389949. Biochem Pharmacol. 2019 Aug;166:163-173. doi: 10.1016/j.bcp.2019.04.030. Epub 2019 May 11. PMID: 31085160. 2: Stalder AK, Lott D, Strasser DS, Cruz HG, Krause A, Groenen PM, Dingemanse J. 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. doi: 10.1111/bcp.13149. Epub 2016 Nov 15. PMID: 27730665; PMCID: PMC5306489. 3: Lupisella J, St-Onge S, Carrier M, Cook EM, Wang T, Sum C, Fernando G, Apgar K, Zhang R, Carson N, Snyder BJ, Ryan CS, Ma X, Dierks EA, Little S, Kick EK, Wurtz NR, Bouvier M, Héroux M, Garcia RA. Molecular Mechanisms of Desensitization Underlying the Differential Effects of Formyl Peptide Receptor 2 Agonists on Cardiac Structure-Function Post Myocardial Infarction. ACS Pharmacol Transl Sci. 2022 Sep 14;5(10):892-906. doi: 10.1021/acsptsci.2c00042. PMID: 36268126; PMCID: PMC9578139. 4: Merlin J, Park J, Vandekolk TH, Fabb SA, Allinne J, Summers RJ, Langmead CJ, Riddy DM. Multipathway In Vitro Pharmacological Characterization of Specialized Proresolving G Protein-Coupled Receptors. Mol Pharmacol. 2022 Apr;101(4):246-256. doi: 10.1124/molpharm.121.000422. Epub 2022 Feb 6. PMID: 35125345. 5: Vergelli C, Khlebnikov AI, Crocetti L, Guerrini G, Cantini N, Kirpotina LN, Schepetkin IA, Cilibrizzi A, Quinn MT, Rossi P, Paoli P, Giovannoni MP. Synthesis, biological evaluation, molecular modeling, and structural analysis of new pyrazole and pyrazolone derivatives as N-formyl peptide receptors agonists. Chem Biol Drug Des. 2021 Oct;98(4):582-603. doi: 10.1111/cbdd.13913. Epub 2021 Jul 1. PMID: 34148303; PMCID: PMC8446315.