906556-51-2

VUF11211 is a potent CXCR3 antagonist. It acts by extending from the minor pocket into the major pocket of the transmembrane domains and binding between residues in helices 1 (Y1.39), 2 (W2.60), 3 (F3.32), 4 (D4.60), 6 (Y6.51), and 7 (S7.39, Y7.43).

VUF11211 is an allosteric inverse CXCR3 agonist with a Kd of 0.65 nM[1].

[1] Scholten DJ, et al. Pharmacological characterization of [3H]VUF11211, a novel radiolabeled small-molecule inverse agonist for the chemokine receptor CXCR3. Mol Pharmacol. 2015 Apr;87(4):639-48. DOI:10.1124/mol.114.095265