Bexotegrast

CAS No. 2376257-44-0

Bexotegrast( —— )

Catalog No. M35169 CAS No. 2376257-44-0

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 190 Get Quote
5MG 434 Get Quote
10MG 750 Get Quote
25MG 1260 Get Quote
50MG 2138 Get Quote
100MG 3436 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Bexotegrast
  • Note
    Research use only, not for human use.
  • Brief 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.
  • Description
    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.
  • In Vitro
    ——
  • In Vivo
    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.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Integrin
  • Recptor
    Integrin
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2376257-44-0
  • Formula Weight
    492.61
  • Molecular Formula
    C27H36N6O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (507.50 mM; Ultrasonic )
  • SMILES
    N([C@@H](CCN(CCCCC=1NC=2C(=CC1)CCCN2)CCOC)C(O)=O)C=3C4=C(N=CN3)C=CC=C4
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Anindya Roy, et al. De novo design of highly selective miniprotein inhibitors of integrins αvβ6 and αvβ8. Nat Commun. 2023 Sep 13;14(1):5660.?
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