詳細信息(中文): SCH 546738是高活性的非競爭性CXCR3拮抗劑,Ki為0.4 nM。 詳細信息(英文): 產品描述:SCH 546738SCH 546738 is a novel, potent and non-competitive small molecule CXCR3 antagonist with Ki of 0.4 nM ._x000D_
IC50 Value: ~1 or 2 nM [1]_x000D_
in vitro: SCH 546738 at 10 nM inhibited T cell chemotaxis induced by all three CXCR3 ligands about 90%. In multiple experiments, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor was determined to be 0.4 nM. 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. 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 [1]. _x000D_
in vivo: 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 mo
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