Ripasudil HCl dihydrate


Catalog No. size PriceQuantity
M6848-2 2mg solid $117
M6848-10 10mg solid $482

Description

Cas:887375-67-9

Product Information

Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

 

Chemical Formula: C15H23ClFN3O4S

 

Exact Mass: 323.1104

 

Molecular Weight: 395.8744

 

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

 

Related CAS #:

223644-02-8 (HCl)   

223645-67-8 (free base)   

887375-67-9 (HCl dihydrate)    

 

Synonym: 

 

K115

K 155

brand name

Glanatec

Ripasudil HCl dihydrate

 

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]

 

Technical Data:

 

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

 

In Vitro:

Ripasudil (K-115) is a potent inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively. Ripasudil also shows less potent inhibitory activities against CaMKIIα, PKACα and PKC, with IC50s of 370 nM, 2.1 μM and 27 μM, respectively. Ripasudil (K-115; 1, 10 μM) induces cytoskeletal changes, including retraction and cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. Ripasudil (5 μM) sifnificantly reduces transendothelial electrical resistance (TEER), and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers.

 

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. 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.

 

 

References

 

  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.

 

  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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

Products are for research use only. Not for human use.

 

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