SCH 546738

SCH 546738 is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3; K_i = 0.4 nM).¹ It is selective for CXCR3 over a panel of 49 other receptors at 10 µM. SCH 546738 (10 or 100 nM) inhibits chemotaxis induced by CXC ligand 9 (CXCL9), CXCL10, or CXCL11 in hemagglutinin- and IL-2-activated primary human T cells. It increases survival in combination with cyclosporin A (Item No. 12088) in a rat model of graft versus host disease (GVHD) when administered at a dose of 5 mg/kg twice per day. SCH 546738 also reduces tumor growth and CD8⁺ T cell tumor infiltration in a murine B16/F10 melanoma model.² It decreases hepatic Cxcr3, thiobarbituric acid reactive substance (TBARS), and triglyceride levels and hepatic macrophage infiltration in a mouse model of metabolic dysfunction-associated steatohepatitis (MASH) induced by a methionine- and choline-deficient diet when administered at a dose of 10 mg/kg per day.³

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1. Jenh, C.-H., Cox, M.A., Cui, L., et al. A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection. BMC Immunol. 13, 2 (2012).

2. Yue, C., Shen, S., Deng, J., et al. STAT3 in CD8⁺ T cells inhibits their tumor accumulation by downregulating CXCR3/CXCL10 axis. Cancer Immunol. Res. 3(8), 864-870 (2015).

3. Zhang, X., Han, J., Man, K., et al. CXC chemokine receptor 3 promotes steatohepatitis in mice through mediating inflammatory cytokines, macrophages and autophagy. J. Hepatol. 64(1), 160-170 (2016).