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Purity: ≥98%
Ripasudil HCl dihydrate (formerly K-115; K-115; trade name: Glanatec), the hydrochloride salt and hydrated form of ripasudil, is a ROCK1/2 inhibitor with antihypertensive effects. It inhibits ROCK1/2 with IC50s of 51 nM and 19 nM, respectively. Ripasudil has been approved in Japan for the treatment of glaucoma and ocular hypertension. In Japan, Ripasudil was used as a 0.4% ophthalmic solution for glaucoma.
| ln Vitro |
Ripasudil (K-115) is a strong inhibitor of ROCK with IC50 values of 19 and 51 nM for ROCK2 and ROCK1, respectively. Ripasudil exhibits mild inhibitory effects on CaMKIIα, PKACα, and PKC, as evidenced by its respective IC50 values of 370 nM, 2.1 μM, and 27 μM [1]. In cultivated trabecular meshwork (TM) cells, ripasudil (K-115; 1, 10 μM) produces cytoskeletal alterations such as cell rounding, shrinkage, and a decrease in actin bundles. In Schlemm's canal endothelial (SCE) cell monolayers, ripasudil (5 μM) dramatically lowers transendothelial electrical resistance (TEER) and raises FITC-dextran permeability [2].
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| ln Vivo |
Intraocular pressure (IOP) is lowered by dipasudil (K-115) in a concentration-dependent manner, with concentrations in rabbit eyes ranging from 0.0625% to 0.5% and in monkey eyes from 0.1% to 0.4%[1]. In retinal ganglion cells (RGCs), dipasudil (K-115; 1 mg/kg, po daily) has a neuroprotective effect following nerve compression (NC). In mice, ripasudil also prevents oxidative stress brought on by axonal damage. Following NC damage, ripasudil inhibits the time-dependent generation of ROS in RGCs[3].
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| 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 |
| Molecular Formula |
C15H18FN3O2S.HCL.2H2O
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|---|---|
| Molecular Weight |
395.88
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| CAS # |
887375-67-9
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| Related CAS # |
223645-67-8
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| SMILES |
FC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2.[H]Cl.O.O
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| Synonyms |
K-115; trade name: Glanatec; K115; K 155; Ripasudil
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (252.60 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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