2. Immunology/Inflammation
  3. Galectin
  4. Galectin-3-IN-6

Galectin-3-IN-6 (Compound 12) 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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Galectin-3-IN-6

Galectin-3-IN-6 Chemical Structure

CAS No. : 2604662-64-6

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Galectin-3-IN-6 Related Antibodies

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Description

Galectin-3-IN-6 (Compound 12) 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[1].

In Vitro

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.

Galectin-3-IN-6 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC
Mice[1] 10 mg/kg p.o. 1540 ng/mL 4460 ng·h/mL
Mice[1] 100 mg/kg p.o. 15400 ng/mL 169000 ng·h/mL
In Vivo

Galectin-3-IN-6 (100 mg/kg; p.o.; twice daily) exhibits robust anti-fibrotic activity in a mouse model of acute CCl4 (HY-Y0298)-induced liver injury and fibrosis, producing median reductions of 64% and 71% in collagen-1 and αSMA levels, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 J (homozygous, Gal-3 V160A point mutation)[1]
Dosage: 100 mg/kg
Administration: p.o.; twice daily
Result: Reduced collagen-1 levels by a median of 64%.
Reduced α-smooth muscle actin (αSMA) levels by a median of 71%.
Molecular Weight

645.45

Formula

C28H29Cl2F3N4O6
CAS No.
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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Purity & Documentation
References
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Galectin-3-IN-6 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Galectin-3-IN-62604662-64-6Galectincollagen-1mouse model of acute liver injury and fibrosismouse liver microsomescarbohydrate recognition domainfibrosisα-smooth muscle actinhuman liver microsomesmutant mouse galectin-3 (V160A)galectin-3acute liver injuryInhibitorinhibitorinhibit

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