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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 | $68 | In Stock | |
| 5 mg | $163 | In Stock | |
| 10 mg | $259 | In Stock | |
| 25 mg | $428 | In Stock | |
| 50 mg | $619 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $177 | 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 integrin:5.7 nM (Kd), αvβ1 integrin: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]. |
| Synonyms | 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/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (203 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.12 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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