Formulation: A solid
Formal Name: (3′S,9S)-5-ethenyl-3R,4,4aR,5S,6,7,8S,8aS-octahydro-1′-methoxy-7-methyl-spiro[3,5,8-ethanylylidene-1H-pyrano[3,4-c]pyridine-10,3′-[3H]indol]-2′(1′H)-one
Purity: ≥98%
Formula Markup: C21H24N2O3
Formula Weight: 352,4
Shelf life (days): 1460
CAS Number: 38990-03-3
Notes: Gelsevirine is an oxindole alkaloid that has been found in G. elegans and has anti-inflammatory activity.{68827,68828} It binds to stimulator of interferon genes (STING; Kd = 27.6 µM) and prevents 2'3'-cGAMP-induced Sting dimerization in RAW 264.7 macrophages when used at a concentration of 5 µM.{68828} Gelsevirine (10 µM) inhibits 2'3'-cGAMP-, poly(dA:dT) dsDNA-, or IFN-stimulatory DNA-induced increases in the levels of mRNA encoding chemokine (C-X-C motif) ligand 10 (CXCL10) and IL-6 in THP-1 monocytes and RAW 264.7 cells. It inhibits 2'3'-cGAMP-induced increases in the levels of Sting and phosphorylated IFN regulatory factor 3 (IRF3), p65, and TANK-binding kinase 1 (TBK1) in RAW 264.7 cells when used at a concentration of 5 µM. In vivo, gelsevirine (20 mg/kg) increases animal survival time, reduces lung injury and total protein levels in bronchoalveolar lavage fluid (BALF), and decreases serum levels of alanine transaminase (ALT), aspartate aminotransferase (AST), creatinine, IL-6, TNF-α, and blood urea nitrogen (BUN) levels in wild-type, but not Sting1-/-, mice in a model of sepsis induced by cecal ligation and puncture (CLP).
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