Cas No.: | 300816-15-3 |
Chemical Name: | RS-504393; RS504393 |
Synonyms: | RS-504393; RS504393 |
SMILES: | O=C1NC2=CC=C(C)C=C2C3(CCN(CCC4=C(C)OC(C5=CC=CC=C5)=N4)CC3)O1 |
Formula: | C25H27N3O3 |
M.Wt: | 417.5002 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively). |
In Vivo: | RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice[1]. 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[2]. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model[3]. |
In Vitro: | RS 504393 inhibits the MCP-1-induced chemotaxis with an IC50 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[4]. |