Gelsevirine

Gelsevirine is an oxindole alkaloid that has been found in G. elegans and has anti-inflammatory activity.1,2 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.2 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).WARNING This product is not for human or veterinary use.

An oxindole alkaloid with anti-inflammatory activity

352.4

≥98%

Biochemicals/Receptor Pharmacology/Antagonists,Natural Products/Alkaloids

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

O=C1[C@]([C@@](OC2)([H])C[C@]3([H])[C@@]2([H])[C@@]4([H])N5C)(C6=CC=CC=C6N1OC)[C@]4([H])[C@]3(C5)C=C

C21H24N2O3

38990-03-3

≥ 4 years

Methanol: Sparingly Soluble: 1-10 mg/ml