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Galectin-3-IN-3 (Compound 4) is an orally active and selective inhibitor of Gal-3, with IC50 values of 11 nM and 84 nM against mGal-3 and hGal-3 respectively[1]. | [in vivo]
Galectin-3-IN-3 (2 mg/kg; i.v.; single dose) exhibits low clearance rate (CL=8 mL/min/kg), high volume of distribution (Vss=1.8 L/kg), and good oral bioavailability (F=40%) in mice plasma[1]. | [IC 50]
hGal-3: 11 nM (IC50); mGal-3: 84 nM (IC50); hGal-1: 2720 nM (IC50); hGal-9: 3530 nM (IC50) | [References]
[1] Liu C, et al. Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design. Bioorg Med Chem. 2024;101:117638. DOI:10.1016/j.bmc.2024.117638 |
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