| Molecular Formula | C25H27N3O3 |
| Molar Mass | 417.5 |
| Density | 1.28 |
| Solubility | DMSO: soluble1mg/mL, clear (warmed) |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | 2-8°C |
| Refractive Index | 1.645 |
| MDL | MFCD09038564 |
| In vitro study | RS 504393 inhibits the MCP-1-induced chemotaxis with an IC 50 of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393. |
| In vivo study | RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice. RS 504393 (5mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model. |
| Hazard Symbols | Xi - Irritant![]() |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.395 ml | 11.976 ml | 23.952 ml |
| 5 mM | 0.479 ml | 2.395 ml | 4.79 ml |
| 10 mM | 0.24 ml | 1.198 ml | 2.395 ml |
| 5 mM | 0.048 ml | 0.24 ml | 0.479 ml |
| biological activity | RS 504393 is a selective CCR2 antagonist that acts on human recombinant CCR2 and CCR1 receptors with IC50 values of 89 nM and> 100 μM respectively. |
| target | CCR2 89 nM (IC 50 ) Human α 1a receptor 72 nM (IC 50 ) Human α 1d receptor 460 nM (IC 50 ) 5HT-1a receptor 1070 nM (IC 50 ) |
| in vitro study | RS 504393 inhibits the MCP-1-induced chemotaxis with an IC 50 of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393. |
| in vivo study | RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in ice. RS 504393 (5 mg/kg, I. v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS. RS-504393 significantly reduces pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model. |