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Galectin-3-IN-4 (compound 5) is a carboxamide analog. Galectin-3-IN-4 is a potent, selective, and orally bioavailable inhibitor of human and mouse galectin-3, with IC50 values of 21 and 167 nM for hGal-3 and mGal-3, respectively. Galectin-3-IN-4 has IC50 values of 1580 and 2750 nM for hGal-1 and hGal-9, respectively[1]. | [in vivo]
Galectin-3-IN-4 (compound 5) (2 mg/kg IV, 10 mg/kg PO; once) has a low clearance rate (CL = 12 mL/min/kg) and a high volume of distribution (Vss = 2.1 L/kg), and has a 52 % oral bioavailabilities in mice[1]. | [IC 50]
Galectin-3: 21 nM (IC50, hGal-3); Galectin-3: 167 nM (IC50, mGal-3); Galectin-1: 1580 nM (IC50, hGal-1) | [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 Mar 1;101:117638. DOI:10.1016/j.bmc.2024.117638 |
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