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Ripasudil(K-115)

  Cat. No.:  DC7774   Featured
Chemical Structure
887375-67-9
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More than 5000 active chemicals with high quality for research!
Field of application
K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 887375-67-9
Chemical Name: Ripasudil hydrochloride dihydrate
Synonyms: K115;K-115 Hydrochloride Dihydrate;Ripasudil;K-115;Ripasudil hydrochloride dihydrate;016TTR32QF;Ripasudil hydrochloride hydrate [JAN];Ripasudil hydrochloride hydrate (JAN);Ripasudil hydrochloride hydrate;Glanatec (TN);Ripasudil hydrochloride dihydrate [WHO-DD];C15H18FN3O2S.ClH.2H2O;BCP11082;s7995;3757AH;1H-1,4-Diazepine, 1-((4-fluoro-5-is
SMILES: Cl[H].S(C1=C([H])C([H])=C([H])C2=C([H])N=C([H])C(=C12)F)(N1C([H])([H])C([H])([H])C([H])([H])N([H])C([H])([H])[C@]1([H])C([H])([H])[H])(=O)=O.O([H])[H].O([H])[H]
Formula: C15H23ClFN3O4S
M.Wt: 395.8772
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
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].
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[1]. 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[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC8329 SLx-2119(KD-025,Belumosudil ) SLx-2119(KD-025) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM)
DC9854 SAR407899 SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
DC7269 RKI-1447 RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.
DC8831 RKI-1313 RKI-1313 is the negative control for RKI-1447 which is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer
DC7774 Ripasudil(K-115) K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.
DC9614 Hydroxyfasudil (hydrochloride) Hydroxyfasudil Hcl(HA1100 Hcl), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
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