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Merck

344149

FPRL1 Agonist II, C43

Synonym(s):

FPRL1 Agonist II, C43, 1-(4-chlorophenyl)-3-(5-isopropyl-1-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)urea, Formyl Peptide Receptor-Like 1 Agonist II, FPR2 Agonist II, ALX Agonist II

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About This Item

Empirical Formula (Hill Notation):
C20H21ClN4O2
CAS Number:
Molecular Weight:
384.86
UNSPSC Code:
12352200
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assay

≥93% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

light brown

solubility

DMSO: 50 mg/mL

shipped in

wet ice

storage temp.

2-8°C

Quality Level

Disclaimer

Toxicity: Standard Handling (A)

General description

An orally available, stable, pyrazolone derivative that acts as a potent prototypic agonist of human formyl-peptide-like 1 receptor (hFPRL1; FPR2) (EC50 = 44 nM). Also shown to block polymorphonuclear neutrophil (PMN) migration in a dose-dependent manner, irrespective of the type of stimulant applied. Reported to act by activating extracellular loop I, while the downstream signaling effects are attributed to its loop II region. Does not affect several other protein targets studied, such as p38a, CXCR2, histamine receptor, and TRPV1 (~10 mM). Exhibit suitable pharmacokinetic properties, such as low clearance (126 ml/h/kg) and a half-life of ~2.78 hours. Shown to significantly reduce edema in mouse ear (~50 mg/kg) following oral administration.

Other Notes

Bena, S., et al. 2012, J Biol Chem287, 24690.
Burli, R. W, et al. 2006, Bioorg Med Chem Lett.16, 3713.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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