Galectin-3-IN-6
Galectin-3-IN-6 is a human and murine galectin-3 (Gal-3) inhibitor, with an IC50 of 12 nM against human galectin-3, an IC50 of 12.6 nM against mutant murine galectin-3 (V160A), and a Kd of 13 nM for human galectin-3, as well as oral bioavailability. Galectin-3-IN-6 reduces the levels of liver fibrosis markers type I collagen and α-smooth muscle actin in mouse models of acute liver injury and fibrosis. Galectin-3-IN-6 can be used for the research of acute liver injury and fibrosis.
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- CAS. Nr.: 2604662-64-6
- Formel: C28H29Cl2F3N4O6
- Molecular Weight:645.45
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Galectin-3 12 nM (IC50) |
Galectin-3 13 nM (Kd) |
Galectin-3-IN-6 (compound 12) potently inhibits human galectin-3 in an asialofetuin competitive binding assay with an IC50 of 12 nM[1].
Galectin-3-IN-6 (compound 12) binds to human galectin-3 with a Kd of 13 nM, as measured by Biacore analysis[1].
Galectin-3-IN-6 (compound 12) exhibits metabolic stability in human and mouse liver microsomes with intrinsic clearance values of 29 and 20 μL/(min*mg), respectively[1].
Galectin-3-IN-6 (compound 12) forms a stable complex with human galectin-3, as confirmed by X-ray crystallography (PDB ID: 8RMT), with its hydroxy group replacing the conserved water in the lectin's carbohydrate recognition domain[1].
Galectin-3-IN-6 (compound 12) binds to V160A mutant mouse galectin-3 with a Kd of 12.6 nM, identical to its inhibitory potency against human galectin-3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 J (homozygous, Gal-3 V160A point mutation)[1]
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Dosage:100 mg/kg
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Administration:p.o.; twice daily
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Result:Reduced collagen-1 levels by a median of 64%.
Reduced α-smooth muscle actin (αSMA) levels by a median of 71%.
Chemical Information
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CAS. Nr. 2604662-64-6
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Molecular Weight 645.45
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Formel C28H29Cl2F3N4O6
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SMILES
FC1=C(F)C(F)=CC(C2=CN([C@@H]3[C@@H](OC)[C@H](C(N(C4=CC(Cl)=CC(Cl)=C4)[C@@H]5[C@@H](O)CCCC5)=O)O[C@H](CO)[C@@H]3O)N=N2)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)