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Merck
CN

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
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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产品名称

Ripasudil Hydrochloride, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear

storage temp.

2-8°C

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

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

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分析证书(COA)

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Yoshio Kaneko et al.
Scientific reports, 6, 19640-19640 (2016-01-20)
Ripasudil hydrochloride hydrate (K-115), a specific Rho-associated coiled-coil containing protein kinase (ROCK) inhibitor, was the first ophthalmic solution developed for the treatment of glaucoma and ocular hypertension in Japan. Topical administration of K-115 decreased intraocular pressure (IOP) and increased outflow
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
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.



全球贸易项目编号

货号GTIN
SML3000-25MG04065265793100
SML3000-5MG04065265793117