reparixin

Description: Reparixin (also known as Repertaxin), is a novel, potent small molecular weight allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. It is the first drug candidate currently under clinical investigation in the prevention of ischemia/reperfusion injury in organ transplantation. Reparixin binding mode to CXCR1 has been studied and used for a computer-assisted design program of dual allosteric CXCR1 and CXCR2 inhibitors. Structural and biochemical data are consistent with a noncompetitive allosteric mode of interaction between CXCR1 and Repertaxin, which, by locking CXCR1 in an inactive conformation, prevents signaling. Repertaxin is an effective inhibitor of polymorphonuclear cell recruitment in vivo and protects organs against reperfusion injury. Targeting the Repertaxin interaction site of CXCR1 represents a general strategy to modulate the activity of chemoattractant receptors.

References: Proc Natl Acad Sci U S A. 2004 Aug 10; 101(32):11791-6; J Med Chem. 2007 Aug 23; 50(17):3984-

Related CAS#: 266359-93-7 (lysine salt); 266359-83-5 (free);