SCH 546738

SCH 546738 is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3, Ki = 0. nM). 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 (Cay-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. 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.. Solulibility: DMSO: Sparingly Soluble: 1-10 mg/ml: .