CAY10746

• CAT Number: I024174
• CAS Number: 2247240-76-0
• Molecular Formula: C26H23N3O5
• Molecular Weight: 457.48
• Purity: ≥95%
• Synonyms: 4-(dimethylamino)-N-[3-[[2-(4-oxochromen-7-yl)oxyacetyl]amino]phenyl]benzamide
• InChI: InChI=1S/C26H23N3O5/c1-29(2)20-8-6-17(7-9-20)26(32)28-19-5-3-4-18(14-19)27-25(31)16-34-21-10-11-22-23(30)12-13-33-24(22)15-21/h3-15H,16H2,1-2H3,(H,27,31)(H,28,32)
• InChIKey: WVGDUQVQWLHVEA-UHFFFAOYSA-N
• SMILES: CN(C)C1=CC=C(C=C1)C(=O)NC2=CC=CC(=C2)NC(=O)COC3=CC4=C(C=C3)C(=O)C=CO4

CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR)[1].
CAY10746 (compound 12j) has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively[1].
CAY10746 (0.1, 1 and 10 μM; 0.25, 1, 2 and 4 h) inhibits ROCK kinase activity in SH-SY5Y cells[1].
CAY10746 (1 μM; 24 h, 36 h) inhibits endothelial cell migration in vitro[1].
CAY10746 (1 μM; 5 days) protects retinal neurons from high glucose-induced oxidative stress and apoptosis-mediated cell death[1].
CAY10746 (1 μM; 5 days) suppresses the improper proliferation of Müller cells and promoted the regression of vascular vessels in retinal explants cultured in a high glucose microenvironment[1].

Reference

[1]. Lanying Zhao, et al. Discovery of 4 H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models. J Med Chem. 2019 Dec 12;62(23):10691-10710.
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