227016
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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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
07 September 2010
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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.
| Product information | |||
|---|---|---|---|
| Form | White solid | ||
| Molar mass | 593.7 | ||
| Protect from Light | Yes | ||
| Hygroscopic | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC (racemic mixture) | ||
| Solubility | DMSO or H2O | ||
| Chemical formula | C28H34F3N5O4S | ||
| CAS number | 445479-97-0 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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| Safety information | |||
|---|---|---|---|
| S Phrase |
S: 22-24/25-36/37/39 Do not breathe dust. Avoid contact with skin and eyes. Wear suitable protective clothing, gloves and eye/face protection. |
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