ALK5-IN-87
ALK5-IN-87 is a potent lung-restricted ALK5 inhibitor with a pKi of 10.13. ALK5-IN-87 exerts antifibrotic activity in a mouse model of lung fibrosis. ALK5-IN-87 can be used for the research of idiopathic pulmonary fibrosis.
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- CAS. Nr.: 2921605-02-7
- Formel: C25H29ClFN7O2S
- Molecular Weight:546.06
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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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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
ALK5-IN-87 (compound 20) inhibits TGF-β1-induced pSMAD2 phosphorylation in A549 cells with a pIC50 of 7.28[1].
ALK5-IN-87 inhibits TGF-β1-induced pSMAD2 phosphorylation in human lung fibroblasts with a pIC50 of 7.69[1].
ALK5-IN-87 potently inhibits purified ALK4 kinase domain with a pKi of 9.86[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CLplasma | Vdss | T1/2 |
|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 70 mL/min/kg | 5.2 L/kg | 1.7 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (7-8 weeks old) with Bleomycin (BLM) (HY-17565)-induced lung fibrosis[1]
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Dosage:0.3; 1 mg/kg
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Administration:i.n.; once daily; starting at day 7 until day 21
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Result:Significantly slowed down the decline in forced vital capacity (FVC) value by 43% at 1 mg/kg, ompared to BLM group.
Did not result in an increased efficacy compared to the lower dose of 1 mg/kg at 0.3 mg/kg.
Induced a significant decrease by 23% in the Ashcroft score compared to the vehicle/BLM-treated animals at 1 mg/kg.
Showed antifibrotic activity.
Chemical Information
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CAS. Nr. 2921605-02-7
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Molecular Weight 546.06
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Formel C25H29ClFN7O2S
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SMILES
O=C(NC1=NC=CC(NC2=CC(C3=CC(Cl)=CC=C3F)=NN=C2SCCO)=C1)CCN4CCN(C)CC4
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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)
ALK5-IN-87 Related Classifications
HY-183950 Related Classifications
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