SCH 546738 is a potent, orally active and non-competitiveCXCR3antagonist, the affinity constant (K_i) of SCH 546738 binding to humanCXCR3receptor 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 using³⁵S radiolabeled SCH 535390 (a sulfonamide analog of the CXCR3 compound series with a K_dof 0.6 nM) as a competitive tracer. In addition, SCH 546738 displaces radiolabeled CXCL10 and CXCL11 from human CXCR3 with IC₅₀ranging 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 IC₉₀about 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 K_d(50-100 pM) for the receptor. The IC₅₀of 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^[1].

SCH 546738 has strong cross-species activities with IC₅₀of 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^[1].

492.44

Solid

C₂₃H₃₁Cl₂N₇O

906805-42-3

Room temperature in continental US; may vary elsewhere.

DMSO : 4.5 mg/mL(9.14 mM;Need ultrasonic)

H₂O :< 0.1 mg/mL(insoluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： corn oil

  Solubility: 1 mg/mL (2.03 mM); Suspended solution; Need ultrasonic and warming