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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Galectin-GB1211
GB1211

Chemical Structure : GB1211

CAS No.: 1978336-95-6

GB1211 (Selvigaltin, GB-1211)

货号: PC-49544Not For Human Use, Lab Use Only.

Selvigaltin (GB1211) is a highly potent, selective and orally active Galectin-3 inhibitor with binding Kd of 25 nM in FP assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Selvigaltin (GB1211) 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.

物理化学性质&存储条件

分子量 533.320
分子式 C19H16BrF3N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-Bromopyridin-3-yl 3-Deoxy-3-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-1-thio-alpha-d-galactopyranoside

参考文献

1. Fredrik R Zetterberg, et al. J Med Chem. 2022 Oct 13;65(19):12626-12638.

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