SML3000
Ripasudil Hydrochloride
≥98% (HPLC), rho-associated protein kinase (ROCK) inhibitor, powder
别名:
4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline hydrochloride, K-115 hydrochloride
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关于此项目
经验公式（希尔记法）:
C15H18FN3O2S · xHCl
化学文摘社编号:
分子量:
323.39 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
Ripasudil Hydrochloride, ≥98% (HPLC)
SMILES string
Fc1c2c(cnc1)cccc2[S](=O)(=O)N3[C@H](CNCCC3)C
InChI
1S/C15H18FN3O2S/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14/h2,4-5,9-11,17H,3,6-8H2,1H3/t11-/m0/s1
InChI key
QSKQVZWVLOIIEV-NSHDSACASA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
A potent and selective rho-associated protein kinase (ROCK) inhibitor with in vivo intraocular pressure (IOP) reducing efficacy.
Ripasudil (K-115) is a more potent and selective rho-associated protein kinase (ROCK) inhibitor (IC50 = 51 nM/ROCK1, 19 nM/ROCK2, 2.1 μM/PKACα, 27 μM/PKC, and 0.37 μM/CaMKII?) than Y-27632 and HA-1077 (Fasudil). Ripasudil demonstrates in vivo efficacy in reducing intraocular pressure (IOP) by stimulating aqueous humour drainage through the trabecular meshwork.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Karly P Garnock-Jones
Drugs, 74(18), 2211-2215 (2014-11-22)
Ripasudil hydrochloride hydrate (Glanatec® ophthalmic solution 0.4 %; hereafter referred to as ripasudil) is a small-molecule, Rho-associated kinase inhibitor developed by Kowa Company, Ltd. for the treatment of glaucoma and ocular hypertension. This compound, which was originally discovered by D.
Seigo Nakabayashi et al.
Experimental eye research, 139, 132-135 (2015-07-22)
Ripasudil (K-115) is a novel Rho kinase inhibitor with a potent intraocular pressure-lowering effect. However, it is unclear whether ripasudil affects the retinal blood flow (RBF). We investigated the effect of ripasudil on feline retinal microcirculation. Ripasudil (5 μM, 50 μM or
Akiko Futakuchi et al.
Experimental eye research, 149, 107-115 (2016-07-11)
The most common cause of glaucoma surgery failure is scar formation induced by activation of wound-healing responses and resultant fibrosis at the surgical site. We investigated the effects of ripasudil, a Rho kinase inhibitor, on activation of human conjunctival fibroblasts
Tomoyuki Isobe et al.
Xenobiotica; the fate of foreign compounds in biological systems, 46(7), 579-590 (2015-12-19)
1. We examined the metabolism of ripasudil (K-115), a selective and potent Rho-associated coiled coil-containing protein kinase (ROCK) inhibitor, by in vitro and in vivo studies. 2. First, we identified metabolites and metabolic enzymes involved in ripasudil metabolism. Species differences were observed
Kotaro Yamamoto et al.
Investigative ophthalmology & visual science, 55(11), 7126-7136 (2014-10-04)
To investigate the effect of K-115, a novel Rho kinase (ROCK) inhibitor, on retinal ganglion cell (RGC) survival in an optic nerve crush (NC) model. Additionally, to determine the details of the mechanism of K-115's neuroprotective effect in vivo and
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