2376257-44-0
Chemical Structure
Bexotegrast
Synonym(s): PLN-74809
- CAS No.: 2376257-44-0
- Formula:C27H36N6O3
- Molecular Weight:492.61
IUPAC Name: (S)-4-((2-methoxyethyl)(4-(1,5,6,7-tetrahydro-1,8-naphthyridin-2-yl)butyl)amino)-2-(quinazolin-4-ylamino)butanoic acid
InChIKey: CWOFQJBATWQSHL-DEOSSOPVSA-N
SMILES: OC([C@H](CCN(CCOC)CCCCC(N1)=CC=C2C1=NCCC2)NC3=NC=NC4=C3C=CC=C4)=O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Bexotegrast | 99.74% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Bexotegrast-d3 | ||||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [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. [Content Brief]
- [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. [Content Brief]
