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SML3000

Sigma-Aldrich

Ripasudil Hydrochloride

≥98% (HPLC)

Sinonimo/i:

4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline hydrochloride, K-115 hydrochloride

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About This Item

Formula empirica (notazione di Hill):
C15H18FN3O2S · xHCl
Numero CAS:
Peso molecolare:
323.39 (free base basis)
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Forma fisica

powder

Condizioni di stoccaggio

desiccated

Colore

white to beige

Solubilità

H2O: 2 mg/mL, clear

Temperatura di conservazione

2-8°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
QSKQVZWVLOIIEV-NSHDSACASA-N

Azioni biochim/fisiol

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


Certificati d'analisi (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
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
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.
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

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