diABZI STING agonist-1 trihydrochloride

Description

diABZI STING agonist-1 is an agonist of the stimulator of interferon genes (STING) pathway. It induces secretion of IFN-β in human peripheral blood mononuclear cells (PBMCs; EC₅₀ = 130 nM). diABZI STING agonist-1 (2.5 mg/kg) increases serum levels of IFN-β, IL-6, TNF, and KC/GROα in wild-type, but not Sting-/-, mice. It inhibits the cytopathic effect of the common cold human coronavirus 229E (HCoV-229E) in infected MRC-5 cells (EC₅₀ = 3 nM). diABZI STING agonist-1 also decreases the level of severe acute respiratory coronavirus 2 (SARS-CoV-2) RNA in primary human bronchial airway epithelial cells in an air-liquid interface assay. It decreases tumor volume and increases survival in a CT26 murine colorectal cancer model when administered at a dose of 3 mg/kg.

Uses

1-[(2E)-4-[5-(Aminocarbonyl)-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-methoxy-1H-benzimidazol-1-yl]-2-buten-1-yl]-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-[3-(4-morpholinyl)propoxy]-1H-benzimidazole-5-carboxamide Hydrochloride (1:3), an amino acid derivatve used in preparation of STING protein.