Ripasudil monohydrochloride dihydrate

• CAT Number: A000100
• CAS Number: 887375-67-9
• Molecular Formula: C15H18FN3O2S • HCl [2H2O]
• Molecular Weight: 395.9
• Purity: ≥95%
• Synonyms: Isoquinoline, 4-​fluoro-​5-​[[(2S)​-​hexahydro-​2-​methyl-​1H-​1,​4-​diazepin-​1-​yl]​sulfonyl]​-​, hydrochloride, hydrate (1:1:2)
• Target: Rho
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• InChIKey: CMDJNMACGABCKQ-XVSRHIFFSA-N
• SMILES: FC1=C2C(C=CC=C2S(N3CCCNC[C@@H]3C)(=O)=O)=CN=C1.Cl.O.O

Ripasudil(cas 887375-67-9) is an inhibitor of Rho-associated protein kinase (ROCK; IC50s = 51 and 19 nM for ROCK-I and ROCK-II, respectively). Formulations containing ripasudil are used to lower intraocular pressure in the context of glaucoma and ocular hypertension.

Reference

1: Isobe T, Ohta M, Kaneko Y, Kawai H. Species differences in metabolism of
ripasudil (K-115) are attributed to aldehyde oxidase. Xenobiotica. 2015 Dec
18:1-12. [Epub ahead of print] PubMed PMID: 26678038.

2: Nakabayashi S, Kawai M, Yoshioka T, Song YS, Tani T, Yoshida A, Nagaoka T.
Effect of intravitreal Rho kinase inhibitor ripasudil (K-115) on feline retinal
microcirculation. Exp Eye Res. 2015 Oct;139:132-5. doi:
10.1016/j.exer.2015.07.008. Epub 2015 Jul 18. PubMed PMID: 26197413.

3: Tanihara H, Inoue T, Yamamoto T, Kuwayama Y, Abe H, Suganami H, Araie M; K-115
Clinical Study Group. Additive Intraocular Pressure-Lowering Effects of the Rho
Kinase Inhibitor Ripasudil (K-115) Combined With Timolol or Latanoprost: A Report
of 2 Randomized Clinical Trials. JAMA Ophthalmol. 2015 Jul;133(7):755-61. doi:
10.1001/jamaophthalmol.2015.0525. PubMed PMID: 25880207.

4: Yamamoto K, Maruyama K, Himori N, Omodaka K, Yokoyama Y, Shiga Y, Morin R,
Nakazawa T. 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. PubMed PMID: 25277230.