Burixafor

Burixafor (TG-0054) is a potent CXCR4 antagonist with a pIC₅₀ of 7.4. Burixafor inhibits the binding of CXCL12 to CXCR4, antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, and blocks the downstream Gαᵢ-mediated inhibitory effect on cAMP signal transduction. Burixafor mobilizes CD34⁺ hematopoietic stem/progenitor cells (HSPC) from the bone marrow to the peripheral blood. Burixafor can be used for research on autologous hematopoietic stem cell transplantation (ASCT)^[1][2]. In Vitro:Burixafor potently displaces CXCL12 from its binding to CXCR4 on HEK293 cells stably expressing SNAP-CXCR4, with a pIC₅₀ of 7.4^[1].
Burixafor potently inhibits CXCL12-induced recruitment of miniGαᵢ to CXCR4 in transiently transfected HEK293 cells, with a pIC₅₀ of 7.7^[1].
Burixafor potently inhibits CXCL12-induced recruitment of β-arrestin2 to CXCR4 in transiently transfected HEK293 cells, with a pIC₅₀ of 8.0^[1].
Burixafor potently reverses CXCL12-mediated, CXCR4-dependent inhibition of cAMP in HEK293 cells stably expressing CXCR4, with a pIC₅₀ of 7.9^[1].
Burixafor acts as a potent inverse agonist on constitutively active CXCR4^N119S mutant in transiently transfected HEK293 cells, with a pIC₅₀ of 7.5^[1]. In Vivo:Burixafor mobilizes mesenchymal stem cells, reduces inflammation, and maintains cardiac systolic function in a porcine myocardial infarction model^[1].
Burixafor decreases acute rejection incidence and suppresses cardiac allograft vasculopathy in a Mycophenolate (HY-B0421)-treated swine heart transplant model^[1].
Burixafor mobilizes hematopoietic stem/progenitor cells in mice, with enhanced efficacy when co-administered with Propranolol (HY-B0573B)^[1].