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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

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.

Warning

Toxicity: Standard Handling (A)