VGX-1027 | Immunomodulator; Cytokine release inhibitor

VGX-1027 (6501-72-0) is an immunomodulator that inhibits secretion of IL-1β, TNF-α, and IL-10 from murine macrophages stimulated with LPS and spares T cell function.¹ Ameliorates the course of acute and chronic immunoinflammatory conditions such as carrageenan-induced pleurisy, LPS-induced lethality, and type II collagen-induced arthritis in mouse models.¹ Prevents spontaneous and accelerated forms of autoimmune diabetes in a NOD mouse model.² Modulates genes involved in LPS-induced Toll-like receptor 4 activation in a mouse Lupus model.³ Displays protective effects in particulate matter-induced acute lung injury by blocking TLR4 signaling.⁴

References/Citations:

1) Stojanovic et al. (2007), In vitro, ex vivo and in vivo immunopharmacological activities of the isooxazoline compound VGX-1027: modulation of cytokine synthesis and prevention of both organ-specific and systemic autoimmune diseases in murine models; Clin. Immunol., 123 311
2) Stosic-Grujisic et al. (2007), A potent immunomodulatory compound, (S,R)-3-Phenyl-4,5-dihydro-5-isoxazole acetic acid, prevents spontaneous and accelerated forms of autoimmune diabetes in NOD mice and inhibits the immunoinflammatory diabetes induced by multiple low doses of streptozotocin in CBA/H mice; J. Pharmacol. Exp. Ther., 320 1038
3) Fagone et al. (2014), VGX-1027 modulates genes involved in lipopolysaccharide-induced Toll-like receptor 4 activation and in a murine model of systemic lupus erythematosus; Immunology, 142 594
4) Xu et al. (2019), Protective effects of VGX-1027 in PM2.5-induced airway inflammation and bronchial hyperresponsiveness; Eur. J, Pharmacol., 842 373