PLN-1474

• CAT Number: I042562
• CAS Number: 2408065-32-5
• Molecular Formula: C24H37N3O4
• Molecular Weight: 431.57
• Purity: ≥95%
• Synonyms: (2S)-2-[(4-methyloxane-4-carbonyl)amino]-9-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)nonanoic acid
• InChI: InChI=1S/C24H37N3O4/c1-24(13-16-31-17-14-24)23(30)27-20(22(28)29)10-6-4-2-3-5-9-19-12-11-18-8-7-15-25-21(18)26-19/h11-12,20H,2-10,13-17H2,1H3,(H,25,26)(H,27,30)(H,28,29)/t20-/m0/s1
• InChIKey: GELVLHVQVRSFAY-FQEVSTJZSA-N
• SMILES: CC1(CCOCC1)C(=O)NC(CCCCCCCC2=NC3=C(CCCN3)C=C2)C(=O)O

PLN-1474 (compound 1) is an orally active and selective ανβ1 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 researching a fibrotic or cirrhotic disease or disorder.
PLN-1474 inhibits ανβ1 and ανβ6 with IC50s of <50 nM by solid phase assay[1].
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].

Reference

[1]. Anderson Kraig, et al. Combination treatment of liver diseases using integrin inhibitors. WO2021127483. 2021.