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Key Documents

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SML3000

Sigma-Aldrich

Ripasudil Hydrochloride

≥98% (HPLC)

Sinónimos:

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

Fórmula empírica (notación de Hill):
C15H18FN3O2S · xHCl
Número de CAS:
223645-67-8
Peso molecular:
323.39 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear

storage temp.

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

InChI key

QSKQVZWVLOIIEV-NSHDSACASA-N

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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
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
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
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