KKL 顾客使用本产品发表的 8 篇科研文献

SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (K_i) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.

The affinity of SCH 546738 binding to human CXCR3 receptor is determined by competition binding analysis using S 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. Competition of human CXCL10 and CXCL11 binding to human CXCR3 by SCH 546738 is determined at various concentrations of [I]hCXCL10 and [I]hCXCL11 around the K_d (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 [I]hCXCL10 (25-500 pM) or [I]hCXCL11 (12.5-250 pM), respectively.

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 [I]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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