RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively).
RS 504393 effectively blocks MCP-1-induced chemotaxis with an IC50 of 330 nM and significantly reduces β-hexosaminidase release induced by allergens. It entirely inhibits mast cell degranulation triggered by MCP-1 without allergen priming[4].
体内研究
Administering RS504393 (0.3-3 μg) alongside CCL2 in mice systematically reduces thermal hyperalgesia in a dose-dependent manner[1].
RS 504393 (5 mg/kg, i.v.) counters the increase in leukocytes and protein content in the bronchoalveolar lavage fluid (BALF) induced by LPS, markedly reducing the expressions of IL-1β and PAI-1 mRNA and proteins. It also significantly mitigates lung edema, fluid accumulation, polymorphonuclear leukocyte accumulation, and bronchial wall thickening triggered by LPS[2].
RS-504393 notably ameliorates renal pathology, especially by diminishing extensive interstitial fibrosis through the reduction of type I collagen synthesis in a unilateral ureteral obstruction (UUO) model[3].
体外研究
RS 504393 effectively blocks MCP-1-induced chemotaxis with an IC50 of 330 nM and significantly reduces β-hexosaminidase release induced by allergens. It entirely inhibits mast cell degranulation triggered by MCP-1 without allergen priming[4].
作用机制
RS-504393 prevent MCP-1 binding by occupying the inter-helical bundle region on the extracellular side of the receptor.
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