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SCH 546738

CAS No. : 906805-42-3

MCE 国际站：SCH 546738

产品活性：SCH 546738 是一种有效、可口服的非竞争性 CXCR3 拮抗剂，结合到人 CXCR3 受体的亲和常数 (K_i) 为 0.4 nM。

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

作用靶点：CXCR

In Vitro: The affinity of SCH 546738 binding to human CXCR3 receptor is determined by competition binding analysis using ³⁵S radiolabeled SCH 535390 (a sulfonamide analog of the CXCR3 compound series with a K_d of 0.6 nM) as a competitive tracer. In addition, SCH 546738 displaces radiolabeled CXCL10 and CXCL11 from human CXCR3 with IC₅₀ ranging from 0.8 to 2.2 nM in a non-competitive manner. SCH 546738 potently and specifically inhibits CXCR3-mediated chemotaxis in human activated T cells with IC₉₀ about 10 nM.

In Vivo: SCH 546738 has strong cross-species activities with IC₅₀ of 1.3 nM, 6.4 nM, 5.9 nM and 4.2 nM in inhibiting the binding of [¹²⁵I]hCXCL10 to CXCR3 of monkey, dog, mouse and rat origin, respectively. SCH 546738 is a selective and potent CXCR3 antagonist with a good PK for in vivo studies.

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