ATX inhibitor 26
ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model.
For research use only. We do not sell to patients.
- CAS No.: 2940248-11-1
- Formula: C18H19Cl2N7O3
- Molecular Weight:452.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Autotaxin 57 nM (IC50) |
ATX inhibitor 26 (Compound 27a) (500 nM) has an excellent inhibitory activity against ATX (94.1% inhibition, IC50: 39.2 nM) and Lysophospholipase D (LysoPLD) (over 90% inhibition, IC50: 57.2 nM) in human plasma[1].
ATX inhibitor 26 (3.0 μM, 12-48 h) significantly suppresses LPC/TGF-β-induced MAPK activation in L132, A549 and WI38 cells[1].
ATX inhibitor 26 (0-6.0 μM, 0.5-6.0 h) dose- and time-dependently regulates the MAPK signaling, reducing the phosphorylation levels of ERK, p38, and JNK at doses ≥0.5 μM within 30 min in L132 cells[1].
ATX inhibitor 26 (3.0 μM, 0-48 h) significantly reduces both basal and TGF-β-induced migration of A549 cells and collagen gel contraction of WI38 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L132 cells
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Concentration:0.1, 0.5, 1.0, 3.0, 6.0 μM
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Incubation Time:0.5, 1.0, 3.0, 6.0 h
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Result:Dose- and time-dependently reduced the phosphorylation levels of ERK, p38, and JNK, with effects observed at dose as low as 0.5 μM and within 30 min of treatment.
Significantly suppressed LPC (1 μM) and TGF-β (5 ng/ml)-induced MAPK pathway activation.
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Cell Line:A549 cells
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Concentration:3.0 μM
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Incubation Time:48 h
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Result:Significantly reduced both basal and TGF-β-induced migration of epithelial cells.
| Species | Dose | Route | Tmax | Plasma Concentration | T1/2 | AUC |
|---|---|---|---|---|---|---|
| Mice | 30 mg/kg | o.a. | 0.5 h | 1093.2 μg/mL | 7.5 h | 3088.3 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male C57BL/6 mice (8 weeks old) were given BLM (1.8 U/kg/mouse) through intratracheal injection to induce pulmonary fibrosis[1].
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Dosage:1 or 2 mg/kg
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Administration:oral gavage (p.o.), once a day for 21 days (7 days prior to BLM administration and 14 days post-BLM), and then collects lung tissue.
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Result:Increased survival of BLM-induced pulmonary fibrosis mice.
Significantly reduced collagen deposition, LPAR1, and p-ERK1/2 expression in pulmonary tissue.
Significantly decreased mRNA levels of α-SMA, Col1A1, and pro-inflammatory markers IL-6, IL-1β, and INF-γ in a BLM-induced pulmonary fibrosis model.
Did not induced significant histopathological abnormalities in the liver, kidney, and spleen and notable changes in serum biochemical marker.
Chemical Information
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CAS No. 2940248-11-1
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Molecular Weight 452.29
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Formula C18H19Cl2N7O3
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SMILES
ClC1=CC(Cl)=CC(COC(N2CCC(C3=NN=C(NCC4=CN=NN4)O3)CC2)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ATX inhibitor 26 Related Classifications
HY-173483 Related Classifications
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