Benzamide, 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]- Chemical Properties

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]- Usage And Synthesis

Uses

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].

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]-(2247240-76-0)Related Product Information

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