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SCH 546738
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SCH 546738
CAS No. : 906805-42-3
MCE 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 (Ki) 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 Kd 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. Competition of human CXCL10 and CXCL11 binding to human CXCR3 by SCH 546738 is determined at various concentrations of [125I]hCXCL10 and [125I]hCXCL11 around the Kd (50-100 pM) for the receptor. The IC50 of SCH 546738 is constant (~1 or 2 nM) and independent of the input concentrations of either [125I]hCXCL10 (25-500 pM) or [125I]hCXCL11 (12.5-250 pM), respectively.
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. In addition, SCH 546738 has a favourable pharmacokinetic profile in rodents, the plasma concentrations of SCH 546738 in Lewis rat and C57BL/6 mouse over 24 hr post-dose. The AUC (0-24 hr) is 7.7 μM.hr in Lewis rat 10 mg/kg (mpk) and is 12.6 μM.hr in C57BL/6 mouse 30 mpk.
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