1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. ATX-IN-3

ATX-IN-3 is an orally active autotaxin (ATX) inhibitor with an IC50 of 46 nM. ATX-IN-3 certainly reduces collagen deposition and ameliorates lung fibrosis in the pulmonary fibrosis mouse model. ATX-IN-3 has good metabolic stability and drug-like properties. ATX-IN-3 can used for the study of idiopathic pulmonary fibrosis (IFP).

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ATX-IN-3

ATX-IN-3 Chemical Structure

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Description

ATX-IN-3 is an orally active autotaxin (ATX) inhibitor with an IC50 of 46 nM. ATX-IN-3 certainly reduces collagen deposition and ameliorates lung fibrosis in the pulmonary fibrosis mouse model. ATX-IN-3 has good metabolic stability and drug-like properties. ATX-IN-3 can used for the study of idiopathic pulmonary fibrosis (IFP)[1].

In Vitro

ATX-IN-3 (Compound 12) endows with promising drug-like properties including favorable metabolic stability (t1/2 = 73.06 min, Clint = 18.97 μL/min/mg) in rat liver microsomes, greatly drug-likeness score (1.24) and ligand lipophilicity efficiency (LLE) value (2.98) [1].

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

In Vivo

ATX-IN-3 (Compound 12) (60 mg/kg, i.g., once daily for 21 days) inhibits the development of Bleomycin (HY-108345)-induced pulmonary fibrosis in mice[1].

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

Animal Model: Bleomycin induced IPF model established in male C57BL/6 mice (6-8 weeks)[1]
Dosage: 60 mg/kg
Administration: Oral gavage (i.g.), once daily for 21 days
Result: Significantly improved fibrosis indicators, reduced collagen deposition and inflammatory infiltration.
Did not change heart, liver, and kidney indexes, and ALT, AST and other indicators are all within the normal range.
Molecular Weight

526.56

Formula

C29H27FN6O3

SMILES

FC1=CC=C(C(N2CC(N3CCC(C4=NC5=C(C=CC(NC(C6=CC=CO6)=O)=C5)N4)CC3)(CC#N)C2)=O)C=C1

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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.

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Product Name:
ATX-IN-3
Cat. No.:
HY-175537
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