Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-
- Product Name
- Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-
- CAS No.
- 2247240-76-0
- Chemical Name
- Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-
- Synonyms
- CAY10746;CAY10746,CAY-10746;4-(Dimethylamino)-N-(3-(2-((4-oxo-4H-chromen-7-yl)oxy)acetamido)phenyl)benzamide;4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-benzamide;Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-
- CBNumber
- CB68343259
- Molecular Formula
- C26H23N3O5
- Formula Weight
- 457.48
- MOL File
- 2247240-76-0.mol
Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]- Property
- Boiling point:
- 664.2±55.0 °C(Predicted)
- Density
- 1.363±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: soluble
- form
- A crystalline solid
- pka
- 12.72±0.70(Predicted)
- color
- Off-white to light yellow
Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]- Chemical Properties,Usage,Production
Biological Activity
CAY10746 is an inhibitor of Rho-associated kinase I (ROCK-I) and ROCK-II (IC50s = 14 and 3 nM, respectively).1 It is selective for ROCK-I and ROCK-II over PKA (IC50 = >10,000 nM) and over 387 recombinant human protein kinases in a panel of 394 kinases (IC50s = >10,000 nM for all) but does inhibit LIM kinase 2 (LIMK2), Aurora A, Aurora B, cGMP-dependent protein kinase 1α (PKG1α), and PKG1β (IC50s = 46, 1,072, 1,239, 517, and 660 nM, respectively). CAY10746 (0.1-10 μM) inhibits phosphorylation of the ROCK target protein MYPT1 in SH-SY5Y cells. It also inhibits migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 1 μM. CAY10746 (1 μM) protects isolated mouse retinal neurons from apoptosis and oxidative stress induced by high glucose in an in vitro model of diabetic retinopathy. It also promotes high glucose-induced vessel regression in mouse retinal explants.
References
1.Zhao, L., Li, Y., Wang, Y., et al.Discovery of 4H-chromen-4-one derivatives as a new class of selective Rho kinase (ROCK) inhibitors, which showed potent activity in ex vivo diabetic retinopathy modelsJ. Med. Chem.62(23)10691-10710(2019)
Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
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