TC 14012 (hydrochloride)

TC 14012 is a peptidomimetic antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC₅₀ = 2.9 nM) and CXCR7 agonist.^1,2 It induces β-arrestin recruitment in HEK293T cells expressing CXCR7 (EC₅₀ = 350 nM).¹ TC 14012 reduces the cytopathic effect of HIV in infected MT-4 cells (EC₅₀ = 0.4 nM) and inhibits HIV entry in vitro in a CXCR4-dependent manner (IC₅₀ = 19.3 nM).³ It inhibits migration induced by chemokine (C-X-C motif) ligand 12 (CXCL12) in MDA-MB-231 breast cancer cells and human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 10 to 1,000 nM.² TC 14012 (10 mg/kg) decreases infarct size in a mouse model of acute myocardial infarction induced by left anterior descending (LAD) coronary artery ligation.⁴