2408065-32-5

2408065-32-5 structure

Name: PLN-1474
Chemical Name: 1,8-Naphthyridine-2-nonanoic acid, 5,6,7,8-tetrahydro-α-[[(tetrahydro-4-methyl-2H-pyran-4-yl)carbonyl]amino]-, (αS)-
CAS Number: 2408065-32-5
Molecular Formula: C₂₄H₃₇N₃O₄
Molecular Weight: 431.58
Catalog: Signaling Pathways Cytoskeleton Integrin
Create Date: 2022-11-13 19:37:36
Modify Date: 2024-09-23 17:59:17
PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder[1].

Name	1,8-Naphthyridine-2-nonanoic acid, 5,6,7,8-tetrahydro-α-[[(tetrahydro-4-methyl-2H-pyran-4-yl)carbonyl]amino]-, (αS)-

Description	PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder[1].
Related Catalog	Research Areas >> Inflammation/Immunology Signaling Pathways >> Cytoskeleton >> Integrin
Target	IC50: ＜50 nM (ανβ1), ＜50 nM (ανβ6)[1]
In Vitro	PLN-1474 inhibits ανβ1 and ανβ6 with IC50s of ＜50 nM by solid phase assay[1].
In Vivo	PLN-1474 (10 μM) decreases the expression level of profibrotic genes, including COL1A1 and TIMP1 in liver[1]. PLN-1474 significantly reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in a mouse model of liver fibrosis[1]. PLN-1474 (6-12 weeks) prophylactically or therapeutically blocks SMAD3 phosphorylation and significantly decreases OHP levels, collagen gene expression, and collagen deposition examined histologically in the CDAHFD NASH mouse model[1].
References	[1]. Anderson Kraig, et al. Combination treatment of liver diseases using integrin inhibitors. WO2021127483. 2021.