Bexotegrast

Research use only, not for human use.

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.

Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung.

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Animal Model:C57BL/6 mice Dosage:100, 250, and 500 mg/kg Administration:Orally; twice daily; from Day 7 to Day 21 Result:Showed a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin (3 units/kg)-challenged mice. Dose-dependently blocked Smad3 phosphorylation.

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Cell Cycle/DNA Damage

Integrin

Integrin

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2376257-44-0

492.61

C27H36N6O3

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (507.50 mM; Ultrasonic )

N([C@@H](CCN(CCCCC=1NC=2C(=CC1)CCCN2)CCOC)C(O)=O)C=3C4=C(N=CN3)C=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years