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MedKoo Cat#: 319681 | Name: Ripasudil HCl dihydrate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ripasudil is discontinued and not available from MedKoo

Chemical Structure

Ripasudil HCl dihydrate
Ripasudil HCl dihydrate
CAS#887375-67-9 (HCl dihydrate)

Theoretical Analysis

MedKoo Cat#: 319681

Name: Ripasudil HCl dihydrate

CAS#: 887375-67-9 (HCl dihydrate)

Chemical Formula: C15H23ClFN3O4S

Exact Mass: 323.1104

Molecular Weight: 395.87

Elemental Analysis: C, 45.51; H, 5.86; Cl, 8.95; F, 4.80; N, 10.61; O, 16.17; S, 8.10

Price and Availability

This product was removed for the commercial reasons.
Related CAS #
223644-02-8 (HCl) 223645-67-8 (free base) 887375-67-9 (HCl dihydrate)
Synonym
K-115; K115; K 155; Ripasudil, brand name: Glanatec; Ripasudil HCl dihydrate
IUPAC/Chemical Name
(S)-4-fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride dihydrate
InChi Key
CMDJNMACGABCKQ-XVSRHIFFSA-N
InChi Code
InChI=1S/C15H18FN3O2S.ClH.2H2O/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;1H;2*1H2/t11-;;;/m0.../s1
SMILES Code
O=S(C1=CC=CC2=C1C(F)=CN=C2)(N3[C@@H](C)CNCCC3)=O.[H]Cl.[H]O[H].[H]O[H]
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# CAS#223644-02-8 (Ripasudil hydrochloride ) CAS#223645-67-8 (Ripasudil free base) CAS#887375-67-9 (Ripasudil hydrochloride dihydrate)

Preparing Stock Solutions

The following data is based on the product molecular weight 395.87 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Kaneko Y, Ohta M, Inoue T, Mizuno K, Isobe T, Tanabe S, Tanihara H. 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. PubMed PMID: 26782355; PubMed Central PMCID: PMC4725980. 2: 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. 3: Okumura N, Okazaki Y, Inoue R, Nakano S, Fullwood NJ, Kinoshita S, Koizumi N. Rho-Associated Kinase Inhibitor Eye Drop (Ripasudil) Transiently Alters the Morphology of Corneal Endothelial Cells. Invest Ophthalmol Vis Sci. 2015 Nov 1;56(12):7560-7. doi: 10.1167/iovs.15-17887. PubMed PMID: 26618648. 4: Feng Y, LoGrasso PV, Defert O, Li R. Rho Kinase (ROCK) Inhibitors and Their Therapeutic Potential. J Med Chem. 2015 Oct 30. [Epub ahead of print] PubMed PMID: 26486225. 5: Nakagawa H, Koizumi N, Okumura N, Suganami H, Kinoshita S. Morphological Changes of Human Corneal Endothelial Cells after Rho-Associated Kinase Inhibitor Eye Drop (Ripasudil) Administration: A Prospective Open-Label Clinical Study. PLoS One. 2015 Sep 14;10(9):e0136802. doi: 10.1371/journal.pone.0136802. eCollection 2015. PubMed PMID: 26367375; PubMed Central PMCID: PMC4569567. 6: Tanihara H, Inoue T, Yamamoto T, Kuwayama Y, Abe H, Fukushima A, Suganami H, Araie M; K-115 Clinical Study Group. One-year clinical evaluation of 0.4% ripasudil (K-115) in patients with open-angle glaucoma and ocular hypertension. Acta Ophthalmol. 2016 Feb;94(1):e26-34. doi: 10.1111/aos.12829. Epub 2015 Sep 4. PubMed PMID: 26338317. 7: 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. 8: 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. 9: Tanihara H, Inoue T, Yamamoto T, Kuwayama Y, Abe H, Suganami H, Araie M; K-115 Clinical Study Group. Intra-ocular pressure-lowering effects of a Rho kinase inhibitor, ripasudil (K-115), over 24 hours in primary open-angle glaucoma and ocular hypertension: a randomized, open-label, crossover study. Acta Ophthalmol. 2015 Jun;93(4):e254-60. doi: 10.1111/aos.12599. Epub 2014 Dec 9. PubMed PMID: 25487877. 10: Garnock-Jones KP. Ripasudil: first global approval. Drugs. 2014 Dec;74(18):2211-5. doi: 10.1007/s40265-014-0333-2. PubMed PMID: 25414122. 11: 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. 12: Isobe T, Mizuno K, Kaneko Y, Ohta M, Koide T, Tanabe S. 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. Epub 2014 Feb 6. PubMed PMID: 24502505. 13: Tanihara H, Inoue T, Yamamoto T, Kuwayama Y, Abe H, Araie M; K-115 Clinical Study Group. Phase 2 randomized clinical study of a Rho kinase inhibitor, K-115, in primary open-angle glaucoma and ocular hypertension. Am J Ophthalmol. 2013 Oct;156(4):731-6. doi: 10.1016/j.ajo.2013.05.016. Epub 2013 Jul 4. PubMed PMID: 23831221. 14: Tanihara H, Inoue T, Yamamoto T, Kuwayama Y, Abe H, Araie M; K-115 Clinical Study Group. Phase 1 clinical trials of a selective Rho kinase inhibitor, K-115. JAMA Ophthalmol. 2013 Oct;131(10):1288-95. doi: 10.1001/jamaophthalmol.2013.323. Erratum in: JAMA Ophthalmol. 2014 Jun;132(6):787. PubMed PMID: 23787820. 15: Hughes CC, Yang YL, Liu WT, Dorrestein PC, La Clair JJ, Fenical W. Marinopyrrole A target elucidation by acyl dye transfer. J Am Chem Soc. 2009 Sep 2;131(34):12094-6. doi: 10.1021/ja903149u. PubMed PMID: 19673475; PubMed Central PMCID: PMC2769490. 16: Jha AR, Pillai SK, York VA, Sharp ER, Storm EC, Wachter DJ, Martin JN, Deeks SG, Rosenberg MG, Nixon DF, Garrison KE. Cross-sectional dating of novel haplotypes of HERV-K 113 and HERV-K 115 indicate these proviruses originated in Africa before Homo sapiens. Mol Biol Evol. 2009 Nov;26(11):2617-26. doi: 10.1093/molbev/msp180. Epub 2009 Aug 10. PubMed PMID: 19666991; PubMed Central PMCID: PMC2760466. 17: Heidemeier H, Moser K. Self-other agreement in job performance ratings: a meta-analytic test of a process model. J Appl Psychol. 2009 Mar;94(2):353-70. doi: 10.1037/0021-9010.94.2.353. PubMed PMID: 19271795. 18: Rohling ML, Faust ME, Beverly B, Demakis G. Effectiveness of cognitive rehabilitation following acquired brain injury: a meta-analytic re-examination of Cicerone et al.'s (2000, 2005) systematic reviews. Neuropsychology. 2009 Jan;23(1):20-39. doi: 10.1037/a0013659. Review. PubMed PMID: 19210030. 19: Chatterjee S, Debenedetti PG, Stillinger FH, Lynden-Bell RM. A computational investigation of thermodynamics, structure, dynamics and solvation behavior in modified water models. J Chem Phys. 2008 Mar 28;128(12):124511. doi: 10.1063/1.2841127. PubMed PMID: 18376947. 20: Dalamaga M, Karmaniolas K, Chavelas C, Liatis S, Matekovits H, Migdalis I. Fusobacterium necrophorum septicemia following Epstein-Barr virus infectious mononucleosis. Anaerobe. 2003 Dec;9(6):285-7. PubMed PMID: 16887713.