[CAS NO. 887375-67-9] Ripasudil
PRODUCTS SPECIFICATIONS [887375-67-9]
DESCRIPTION [887375-67-9]
Overview
| MDL | MFCD26960897 |
|---|---|
| Molecular Weight | 395.88 |
| Molecular Formula | C15H23ClFN3O4S |
| SMILES | FC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2.[H]Cl.O.O |
2 Publications Citing Use of MCE
Summary
IC50 & Target
|
ROCK2 19 nM (IC 50 ) |
ROCK1 51 nM (IC 50 ) |
CaMKIIa 370 nM (IC 50 ) |
PKACa 2.1 μM (IC 50 ) |
PKC 27 μM (IC 50 ) |
In Vitro
Ripasudil (K-115) is a potent inhibitor of ROCK, with IC 50 s of 19 and 51 nM for ROCK2 and ROCK1, respectively. Ripasudil also shows less potent inhibitory activities against CaMKIIα, PKACα and PKC, with IC 50 s 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05528172 | Kowa Research Institute, Inc. |
Corneal Edema After Cataract Surgery
|
August 4, 2022 | Phase 3 |
| NCT04621136 | Kyushu University |
Retinopathy of Prematurity
|
November 1, 2020 | Phase 1|Phase 2 |
| NCT05275972 | Stanford University|Oregon Health and Science University|University of California, San Francisco|University of California, Davis|Case Western Reserve University|Dartmouth-Hitchcock Medical Center|University of Pennsylvania |
Fuchs|Fuchs Dystrophy|Fuchs´ Endothelial Dystrophy
|
July 15, 2022 | Phase 3 |
| NCT03249337 | Marian Macsai, MD|NorthShore University HealthSystem |
Fuchs´ Endothelial Dystrophy
|
December 6, 2017 | Phase 4 |
| NCT04620135 | Aerie Pharmaceuticals |
Primary Open Angle Glaucoma|Ocular Hypertension
|
November 12, 2020 | Phase 3 |
| NCT05289661 | Stanford University|Oregon Health and Science University|University of California, San Francisco|University of California, Davis|Case Western Reserve University|Dartmouth-Hitchcock Medical Center|University of Pennsylvania |
Fuchs
|
July 15, 2022 | Phase 3 |
| NCT03575130 | University of Erlangen-Nürnberg Medical School |
Fuchs´ Endothelial Dystrophy|Fuchs Dystrophy|Corneal Endothelial Dystrophy|Corneal Endothelial Cell Loss|Cornea Guttata
|
June 5, 2018 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : ≥ 50 mg/mL ( 126.30 mM )
DMSO : 25 mg/mL ( 63.15 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5260 mL | 12.6301 mL | 25.2602 mL |
| 5 mM | 0.5052 mL | 2.5260 mL | 5.0520 mL |
| 10 mM | 0.2526 mL | 1.2630 mL | 2.5260 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (252.60 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (3.16 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.25 mg/mL (3.16 mM); Clear solution
References
- [1] Isobe T, et al. Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr Eye Res. 2014 Aug;39(8):813-22.
- [2] Kaneko Y, et al. 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.
- [3] Yamamoto K, et al. 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.