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Chemical Structure : GB1211
Catalog No.: PC-49544Not For Human Use, Lab Use Only.
GB1211 (GB-1211) is a highly potent, selective and orally active Galectin-3 inhibitor with binding Kd of 25 nM in FP assays.
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GB1211 (GB-1211) is a highly potent, selective and orally active Galectin-3 inhibitor with binding Kd of 25 nM in FP assays.
GB1211 displays >100-fold selectivity over Galectin-1 as well as low CYP P450 inhibition, also shows no affinity against a panel of 87 different targets (enzymes, receptors, and ion channels).
GB1211 inhibits galectin-3 expression in human monocyte THP1 cells with IC50 of 220.3 nM, inhibits TGFβ stimulated pro-fibrotic gene expression in human liver stellate cell line (LX2) in vitro.
GB1211 (2 mg/kg or 10 mg/kg bid, oral) reduces fibrosis in mouse CCl4-induced liver fibrosis model.
GB1211 is currently in clinical development as a novel, orally active therapy for liver fibrosis.
| M.Wt | 533.320 | |
| Formula | C19H16BrF3N4O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Fredrik R Zetterberg, et al. J Med Chem. 2022 Oct 13;65(19):12626-12638.
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