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RS 504393

CAS No. : 300816-15-3

MCE 站：RS 504393

产品活性：RS 504393 是一种选择性的 CCR2 拮抗剂，作用于人重组 CCR2 和 CCR1 受体，IC₅₀ 值分别为 89 nM 和 > 100 μM。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CCR

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.

In Vivo: RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice. 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 renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Endocrinology Compound Library  |  Pyroptosis Compound Library  |  Pirfenidone  |  Maraviroc  |  INCB3344  |  PF-4136309  |  Bindarit  |  BX471  |  TAK-779  |  RS102895 hydrochloride  |  AZ084  |  CCR6 inhibitor 1  |  CCR2-RA-[R]  |  7,4'-Dihydroxyflavone  |  TAK-220  |  INCB 3284  |  CCR2 antagonist 4 hydrochloride  |  J-113863  |  DAPTA  |  Vicriviroc maleate  |  K777  |  LMD-009  |  SB297006  |  ZK756326 dihydrochloride  |  CCR2 antagonist 3  |  AZD2423  |  CCR2 antagonist 1  |  YM022

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