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227016

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:
445479-97-0
Molecular Weight:
593.66
MDL number:
MFCD00133899
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (racemic mixture, HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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Product Name

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

Quality Level

100

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

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Gentle warming, rapid stirring, and/or sonication may be required for complete solubilization.

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Global Trade Item Number

SKUGTIN
227016-5MG04055977200553