2412688-16-3
Chemical Structure
MORF-627
- CAS No.: 2412688-16-3
- Formula:C31H40FN3O4
- Molecular Weight:537.67
IUPAC Name: (S)-2-(5-fluoro-2-((S)-5-oxaspiro[2.5]octan-6-yl)phenyl)-2-((R)-3-(4-(1,5,6,7-tetrahydro-1,8-naphthyridin-2-yl)butoxy)pyrrolidin-1-yl)acetic acid
InChIKey: PFCLAPQUIKLTKZ-KGPYPHOUSA-N
SMILES: OC([C@@H](N1C[C@@H](CC1)OCCCCC(N2)=CC=C3C2=NCCC3)C4=C(C=CC(F)=C4)[C@@H]5CCC6(CO5)CC6)=O
Biological Activity: MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety[1][2][3].
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MORF-627 | MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety. | |||||||||||||||||||||
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- [1]. Harrison BA, et al. The Discovery of MORF-627, a Highly Selective Conformationally-Biased Zwitterionic Integrin αvβ6 Inhibitor for Fibrosis. J Med Chem. 2024;67(21):18656-18681. [Content Brief]
- [2]. Golovina EL, et al. Therapeutic Prospects of αv Integrins Inhibition in Fibrotic Lung Diseases and Carcinogenesis. Int J Mol Sci. 2025;26(13):6202. Published 2025 Jun 27. [Content Brief]
- [3]. Guffroy M, et al. Selective inhibition of integrin αvβ6 leads to rapid induction of urinary bladder tumors in cynomolgus macaques. Toxicol Sci. 2023;191(2):400-413. [Content Brief]
Keywords
