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Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibiting αvβ6 and αvβ1-induced activation of TGF-β. It is applicable for studies of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $125 | In Stock | |
5 mg | $457 | In Stock | |
10 mg | $789 | In Stock | |
25 mg | $1,370 | In Stock | |
50 mg | $2,324 | In Stock | |
100 mg | $3,818 | In Stock |
Description | Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibiting αvβ6 and αvβ1-induced activation of TGF-β. It is applicable for studies of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP). |
Targets&IC50 | αvβ6:5.7 nM (Kd), αvβ1:3.4 nM (Kd) |
In vitro | Bexotegrast (PLN-74809; 1.82 µM; incubation for 7 days) inhibits lung collagen deposition and Smad3 phosphorylation in a dose-dependent manner[2]. |
In vivo | Bexotegrast(PLN-74809;100–500 mg/kg), administered orally to mice 7 to 21 days after bleomycin-induced lung injury, dose-dependently reduces interstitial fibrotic collagen deposition caused by bleomycin and blocks Smad3 phosphorylation [2]. |
Alias | PLN-74809 |
Molecular Weight | 492.61 |
Formula | C27H36N6O3 |
Cas No. | 2376257-44-0 |
Smiles | N([C@@H](CCN(CCCCC=1NC=2C(=CC1)CCCN2)CCOC)C(O)=O)C=3C4=C(N=CN3)C=CC=C4 |
Storage | keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (202.83 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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