| Identification | Back Directory | [Name]
Ripasudil | [CAS]
223645-67-8 | [Synonyms]
CS-1564
Ripasudil
k115 free base
K-115, Ripasudil
RIPASUDIL HYDROCHLOIDE
RIPASUDIL FREE BASE;K 115 FREE BASE;K115 FREE BASE
4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline
Isoquinoline, 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]- | [Molecular Formula]
C15H18FN3O2S | [MDL Number]
MFCD28291829 | [MOL File]
223645-67-8.mol | [Molecular Weight]
323.39 |
| Chemical Properties | Back Directory | [Description]
Ripasudil (Glanatec TM, Kowa Pharmaceutical), a close derivative of fasudil, is another Rho kinase inhibitor approved in Japan at the end of 2014 for the treatment of glaucoma and ocular hypertensionwhen other therapeutic agents are not effective or cannot be administered. Additionally, ripasudil has been tested in diabetic retinopathy clinical trials and shown to promote corneal endothelial cell proliferation, endothelium regeneration, and wound healing. | [Boiling point ]
497.2±55.0 °C(Predicted) | [density ]
1.293±0.06 g/cm3(Predicted) | [storage temp. ]
under inert gas (nitrogen or Argon) at 2–8 °C | [solubility ]
Soluble in DMSO | [form ]
powder | [pka]
9.70±0.40(Predicted) | [color ]
white to beige | [Water Solubility ]
H2O: 2mg/mL, clear | [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 | [InChIKey]
QSKQVZWVLOIIEV-NSHDSACASA-N | [SMILES]
Fc1c2c(cnc1)cccc2[S](=O)(=O)N3[C@H](CNCCC3)C |
| Hazard Information | Back Directory | [Uses]
Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively. | [Definition]
ChEBI: Ripasudil is a member of isoquinolines. | [in vivo]
Ripasudil (K-115) reduces intraocular pressure (IOP) in a concentration-dependent manner at concentrations between 0.1% and 0.4% in monkey eyes and 0.0625% to 0.5% in rabbit eyes, respectively[1]. Ripasudil (K-115; 1 mg/kg, p.o. daily) shows a neuroprotective effect on retinal ganglion cells (RGCs) after nerve crush (NC). Ripasudil also inhibits the oxidative stress induced by axonal injury in mice. Ripasudil suppresses the time-dependent production of ROS in RGCs after NC injury[3]. | [IC 50]
ROCK2: 19 nM (IC50); ROCK1: 51 nM (IC50); CaMKIIa: 370 nM (IC50); PKACa: 2.1 μM (IC50); PKC: 27 μM (IC50) | [References]
[1] Isobe T, et al. Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr Eye Res. 2014 Aug;39(8):813-22. DOI:10.3109/02713683.2013.874444
[2] Kaneko Y, et al. Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells. Sci Rep. 2016 Jan 19;6:19640. DOI:10.1038/srep19640
[3] Yamamoto K, et al. The novel Rho kinase (ROCK) inhibitor K-115: a new candidate drug for neuroprotective treatment in glaucoma. Invest Ophthalmol Vis Sci. 2014 Oct 2;55(11):7126-36. DOI:10.1167/iovs.13-13842 |
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