Bexotegrast

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 Specifications

CAS Number

[2376257-44-0]

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.