J-113863,353791-85-2

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J-113863

CAS No. : 353791-85-2

MCE 国际站：J-113863

产品活性：J-113863 是一种有效的选择性的 CCR1 拮抗剂，对人和小鼠 CCR1 受体的 IC₅₀ 值分别为 0.9 nM 和 5.8 nM。J-113863 是人 CCR3 的强效拮抗剂 (IC₅₀ 为 0.58 nM)，还是小鼠 CCR3 的弱效拮抗剂 (IC₅₀ 为 460 nM)。J-113863 对 CCR2，CCR4 和 CCR5 以及 LTB4 或 TNF-α 受体没有活性。抗炎作用。

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

作用靶点：CCR

In Vitro: Modified Vaccinia virus Ankara (MVA) but not MVA and vaccinia virus (VACV) infected MH-S cells increase the expression of the CXCR2 acting chemokine CXCL2. MH-S cells constitutively produce CCL2 and CCR1 acting chemokines CCL3, CCL5 and CCL9. Consequently, supernatants of mock treated and virus infected MH-S cells induce chemotaxis of murine promyelocyte MPRO cells and human monocytic THP-1 cells at the same level. However, supernatants of MVA infected MH-S cells significantly increase chemotaxis of the CCR2 deficient human monocytic cell line U-937. Chemotaxis of all above cell types is inhibited by J-113863.

In Vivo: J-113863 (3-10 mg/kg; intraperitoneal injection; once daily; for 11 days; DBA-1 male mice) treatment improves paw inflammation and joint damage, and dramatically decreases cell infiltration into joints in arthritic mice.

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