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A number of Rho kinase inhibitors are known. [15] [16] [17]Chemical structure of fasudil. AT-13148 [18]; BA-210; β-ElemeneBelumosudil; Chroman 1 [19] [20]; DJ4, which is a selective multi-specific ATP competitive inhibitor of activity of ROCK1 (IC50 of 5 nM), ROCK2 (IC50 of 50 nM), MRCKα (IC50 of 10 nM) and MRCKβ (IC50 of 100 nM) kinases without affecting activity of PAK1 and DMPK at 5 μM ...
It is a selective rho-associated coiled-coil-containing protein kinase 1 (ROCK1) inhibitor, where ROCK1 is "an important downstream effector of Rho guanosine trisphosphates (GTP)," [2] proteins that are significant in the contractile control of smooth muscle tissue. The S configuration at the 2-position on the 1,4-diazepane ring of Ripasudil is ...
Netarsudil, sold under the brand name Rhopressa among others, is a medication for the treatment of glaucoma. [1] [2] [3] In the United States, in December 2017, the Food and Drug Administration (FDA) approved a 0.02% ophthalmic solution for the lowering of elevated intraocular pressure in people with open-angle glaucoma or ocular hypertension.
Netarsudil/latanoprost, sold under the brand name Rocklatan among others, is a fixed-dose combination medication use to treat elevated intraocular pressure (IOP) in people with open-angle glaucoma or ocular hypertension. [1] [2] It contains netarsudil mesylate and latanoprost. [1] [2] It is applied as eye drops to the eyes. [1] [2]
Rho kinase inhibitors When comparing people with primary open-angle glaucoma and ocular hypertension, medical intraocular pressure lowering treatment slowed down the progression of visual field loss. [ 4 ]
Rho-associated protein kinase or Rho-associated coiled-coil kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine specific protein kinases. It is involved mainly in regulating the shape and movement of cells by acting on the cytoskeleton .
RKI-1447 is a drug which acts as a potent and selective inhibitor of the enzyme Rho kinase, with an IC 50 of 14.5 nM at ROCK1 and 6.2 nM at ROCK2. It has been investigated for applications in cancer treatment, [ 1 ] [ 2 ] [ 3 ] as well as glaucoma , [ 4 ] and nonalcoholic fatty liver disease .
Verosudil (AR-12286) is a drug which acts as a potent and selective inhibitor of the enzyme Rho kinase, and has been investigated for the treatment of glaucoma. [ 1 ] [ 2 ] See also
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