Bexotegrast

• 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[1][2].

• Product Name Alternative:

  PLN-74809

• UNSPSC:

  12352005

• Target:

  Integrin

• Type:

  Reference compound

• Related Pathways:

  Cytoskeleton

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/bexotegrast.html

• Purity:

  99.74

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  OC ([C@H] (CCN (CCOC) CCCCC (N1) =CC=C2C1=NCCC2) NC3=NC=NC4=C3C=CC=C4) =O

• Molecular Formula:

  C27H36N6O3

• Molecular Weight:

  492.61

• References & Citations:

  [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.|[2]Martin L Decaris, et al. Dual inhibition of αvβ6 and αvβ1 reduces fibrogenesis in lung tissue explants from patients with IPF. Respir Res. 2021 Oct 19;22 (1) :265.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture and light)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  αvβ1; αvβ6

• CAS Number:

  2376257-44-0