Ripasudil HCl dihydrate


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

Description

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

Product information

CAS Number: 887375-67-9

Molecular Weight: 395.88

Formula: C15H23ClFN3O4S

Synonym:

K115

Glanatec

Ripasudil HCl dihydrate

Related CAS Number:

223644-02-8 (HCl)

223645-67-8 (free base)

Chemical Name: (S)-4-fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride dihydrate

Smiles: O.O.Cl.C[C@H]1CNCCCN1S(=O)(=O)C1=CC=CC2=CN=CC(F)=C21

InChiKey: CMDJNMACGABCKQ-XVSRHIFFSA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.
  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. 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.

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

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