1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. ATX-IN-28

ATX-IN-28 is an orally active autotaxin (ATX) inhibitor with an IC50 of 13.7 nM. ATX-IN-28 downregulates the expression of pro-fibrotic α-SMA, ameliorates pathological damage of lung tissues in a bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, and reduces collagen deposition. ATX-IN-28 can be used for research related to idiopathic pulmonary fibrosis.

For research use only. We do not sell to patients.

ATX-IN-28

ATX-IN-28 Chemical Structure

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Description

ATX-IN-28 is an orally active autotaxin (ATX) inhibitor with an IC50 of 13.7 nM. ATX-IN-28 downregulates the expression of pro-fibrotic α-SMA, ameliorates pathological damage of lung tissues in a bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, and reduces collagen deposition. ATX-IN-28 can be used for research related to idiopathic pulmonary fibrosis[1].

In Vitro

ATX-IN-28 (Compound 16) exhibits excellent metabolic stability in pooled male rat liver microsomes, with a half-life of 36.16 min and an intrinsic clearance rate of 38.33 μL/min/mg[1].

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

In Vivo

ATX-IN-28 (Compound 16) (30-60 mg/kg; p.o.; once daily; 15 days) exhibits dose-dependent anti-fibrotic efficacy in bleomycin-induced pulmonary fibrosis in male C57BL/6 mice[1].

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

Animal Model: C57BL/6 (male; bleomycin-induced pulmonary fibrosis model)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; once daily; 15 days
Result: Achieved a modified Ashcroft score of 2.50 via H&E staining and 1.50 via Masson staining.
Decreased lung α-SMA expression to 37.28%.
Reduced BALF ATX activity with a relative absorbance reduction of 3.13 vs. model group, superior to positive control.
Significantly improved lung pathological injury and reduced collagen deposition.
Achieved a modified Ashcroft score of 1.50 via H&E staining and 1.50 via Masson staining.
Decreased lung α-SMA expression to 25.36%.
Mitigated body weight loss and improved survival rate compared to the model group.
Molecular Weight

548.60

Formula

C30H28N8O3

SMILES

O=C(C1=NN(C2=CN(C(C)C)N=C2)C3=C1CCN(C4=CC=CC=C4)C3=O)NC5=CC=CC(/C=C(C#N)/C(NC)=O)=C5

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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-28
Cat. No.:
HY-184278
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