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227016

Sigma-Aldrich

CCR2 Antagonist

≥97% (racemic mixture, HPLC), solid, CCR2 antagonist, Calbiochem®

Synonym(s):

CCR2 Antagonist, 2-((Isopropylaminocarbonyl)amino)-N-(2-((cis-2-((4-(methylthio)benzoyl)amino)cyclohexyl)amino)-2-oxoethyl)-5-(trifluoromethyl)-benzamide, CC Chemokine Receptor 2 Antagonist

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About This Item

Empirical Formula (Hill Notation):
C28H34F3N5O4S
CAS Number:
Molecular Weight:
593.66
UNSPSC Code:
12352200
NACRES:
NA.77

product name

CCR2 Antagonist, The CCR2 Antagonist, also referenced under CAS 445479-97-0, controls the biological activity of CCR2.

Quality Level

Assay

≥97% (racemic mixture, HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

white

solubility

ethanol: 6 mg/mL
DMSO: 60 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

A cis-diamidocyclohexyl urea compound that potently competes against MCP-1 binding to CCR2 (IC50 = 5.1 nM) and effectively inhibits MCP-1/CCR2-mediated PBMCs Ca+2 flux and chemotaxis (IC50 = 18 and 1 nM, respectively), while showing much less effect against eotaxin binding to CCR3 (37% inhibition at 10 µM). Mutageneis analysis indicates CCR2 Thr292 is critical in maintaining the high affinity antagonist binding.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Preparation Note

Gentle warming, rapid stirring, and/or sonication may be required for complete solubilization.

Reconstitution

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

Other Notes

Cherney, R.J., et al. 2008. J. Med. Chem.51, 721.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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