1978336-95-6
Chemical Structure
Selvigaltin
Synonym(s): GB1211
- CAS No.: 1978336-95-6
- Formula:C19H16BrF3N4O4S
- Molecular Weight:533.32
IUPAC Name: (2R,3R,4S,5R,6R)-2-((5-bromopyridin-3-yl)thio)-6-(hydroxymethyl)-4-(4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl)tetrahydro-2H-pyran-3,5-diol
InChIKey: FNCLKJPMEFPXOR-QFACEVIFSA-N
SMILES: O[C@@H]([C@H](O1)SC2=CN=CC(Br)=C2)[C@](N3C=C(C(C=C4F)=CC(F)=C4F)N=N3)([H])[C@H]([C@H]1CO)O
Biological Activity: Selvigaltin (GB1211) is an orally active galectin-3 small molecule inhibitor with an IC50 value of 12 nM in rabbits, showing anti-tumor activity. Selvigaltin decreases galectin-3 levels in the liver and reduces biomarkers of liver function (AST, ALT, bilirubin), inflammation (cells foci) and fibrosis (PSR, SHG), as well as decreasing the mRNA and protein expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen). Selvigaltin restores T-cell activity and induces less tumors and metastasis[1][2][3][4].
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Selvigaltin | 99.89% | Selvigaltin (GB1211) is an orally active galectin-3 small molecule inhibitor with an IC50 value of 12 nM in rabbits, showing anti-tumor activity. Selvigaltin decreases galectin-3 levels in the liver and reduces biomarkers of liver function (AST, ALT, bilirubin), inflammation (cells foci) and fibrosis (PSR, SHG), as well as decreasing the mRNA and protein expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen). Selvigaltin restores T-cell activity and induces less tumors and metastasis. | ||||||||||||||||||||
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- [1]. Slack RJ, et al. The therapeutic potential of galectin-3 inhibition in fibrotic disease. Int J Biochem Cell Biol. 2021 Jan;130:105881. [Content Brief]
- [2]. Zetterberg Fredrik, et al. Preparation of galactosides as galectins inhibitors. WO2020078808+A1. 2020 April 23.
- [3]. Comeglio P, et al. The galectin-3 inhibitor selvigaltin reduces liver inflammation and fibrosis in a high fat diet rabbit model of metabolic-associated steatohepatitis. Front Pharmacol. 2024 Jul 31;15:1430109. [Content Brief]
- [4]. Aslanis V, et al. Single‑Dose Pharmacokinetics and Safety of the Oral Galectin‑3 Inhibitor, Selvigaltin (GB1211), in Participants with Hepatic Impairment. Clin Drug Investig. 2024 Oct 2. [Content Brief]
Keywords
