| Identification | Back Directory | [Name]
α-D-Galactopyranoside, 5-bromo-3-pyridinyl 3-deoxy-1-thio-3-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]- | [CAS]
1978336-95-6 | [Synonyms]
GB-1211
selvigaltin
α-D-Galactopyranoside, 5-bromo-3-pyridinyl 3-deoxy-1-thio-3-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]- | [Molecular Formula]
C19H16BrF3N4O4S | [MOL File]
1978336-95-6.mol | [Molecular Weight]
533.32 |
| Chemical Properties | Back Directory | [Boiling point ]
743.7±70.0 °C(Predicted) | [density ]
1.88±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.40±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Selvigaltin (30 mg/kg, p.o., daily for 5 days) reduces the high fat diet (HFD)-induced increase in plasma cholesterol, ALT plasma levels, collagen deposition, fibrosis and normalize plasma triglycerides levels in HFD rabbits[3].
Selvigaltin (0.3, 1.0, and 5.0 mg/kg, p.o., daily for 4-week) reduces the AST, ALT, bilirubin levels and reduces the HFD-induced increase of several inflammation markers, particularly the mRNA expression of IL6 in HFD rabbits[3].
| Animal Model: | HFD rabbits[3] | | Dosage: | 30 mg/kg | | Administration: | p.o., daily for 5 days | | Result: | Reduced biomarkers of liver function (AST, ALT, bilirubin) and the expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen) in HFD rabbits |
| [IC 50]
Galectin-3 | [References]
[1] Slack RJ, et al. The therapeutic potential of galectin-3 inhibition in fibrotic disease. Int J Biochem Cell Biol. 2021 Jan;130:105881. DOI:10.1016/j.biocel.2020.105881
[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. DOI:10.3389/fphar.2024.1430109
[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. DOI:10.1007/s40261-024-01395-7 |
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