Ripasudil hydrochloride dihydrate

製品コードS7995 バッチS799501

印刷

化学情報

Synonyms

K-115 hydrochloride dihydrate

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₁₈FN₃O₂S.Cl H.2 H₂ O

分子量

395.88

CAS No.

887375-67-9

Solubility (25°C)*

体外

Water

79 mg/mL (199.55 mM)

DMSO (warmed with 50ºC water bath)

26 mg/mL (65.67 mM)

Ethanol (warmed with 50ºC water bath)

5 mg/mL (12.63 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.320mg/ml (3.33mM)
	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.650mg/ml (1.64mM)

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Ripasudil hydrochloride dihydrateは1種の有効な ROCK 阻害剤です。ROCK1 と ROCK2に作用するIC50値は51 nM と 19 nMそれぞれに分かれます。Ripasudil (K-115)は緑内障と高眼圧症の治療に使います。
in vitro	In monkey trabecular meshwork (TM) cells, Ripasudil induces retraction and rounding of cell bodies as well as disruption of actin bundles. In Schlemm's canal endothelial (SCE) cells, Ripasudil significantly decreases transendothelial electrical resistance (TEER), increases the transendothelial flux of FITC-dextran, and disrupts cellular localization of ZO-1 expression.
in vivo	In albino rabbits and monkeys, topical instillation of Ripasudil significantly reduces intraocular pressure (IOP) with maximum IOP reduction of 8.55 mmHg and 4.36 mmHg at 0.5 % and 0.4%, respectively. Ripasudil (1 mg/kg daily, p.o.) exerts a neuroprotective effect on retinal ganglion cell (RGC) after optic nerve crush (NC) by suppressing oxidative stress through pathways involving the Nox family in a mouse model.

製品説明

Ripasudil hydrochloride dihydrateは1種の有効な ROCK 阻害剤です。ROCK1 と ROCK2に作用するIC50値は51 nM と 19 nMそれぞれに分かれます。Ripasudil (K-115)は緑内障と高眼圧症の治療に使います。

in vitro

In monkey trabecular meshwork (TM) cells, Ripasudil induces retraction and rounding of cell bodies as well as disruption of actin bundles. In Schlemm's canal endothelial (SCE) cells, Ripasudil significantly decreases transendothelial electrical resistance (TEER), increases the transendothelial flux of FITC-dextran, and disrupts cellular localization of ZO-1 expression.

in vivo

In albino rabbits and monkeys, topical instillation of Ripasudil significantly reduces intraocular pressure (IOP) with maximum IOP reduction of 8.55 mmHg and 4.36 mmHg at 0.5 % and 0.4%, respectively.

Ripasudil (1 mg/kg daily, p.o.) exerts a neuroprotective effect on retinal ganglion cell (RGC) after optic nerve crush (NC) by suppressing oxidative stress through pathways involving the Nox family in a mouse model.

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase Inhibition Assay
キナーゼアッセイ	ROCK 1 (0.75 ng/μL) and ROCK 2 (0.5 ng/μL) are incubated with various concentrations of K-115, Y-27632, or HA-1077 at 25 °C for 90 min in 50 mmol/L Tris-HCl buffer (pH 7.5) containing 100 mmol/L KCl, 10 mmol/L MgCl₂, 0.1 mmol/L EGTA, 30 μmol/L Long S6 Kinase Substrate peptide, and 1 μmol/L ATP in a total volume of 40 μL. PKACα, PKC, and CaMKIIα are also incubated with various concentrations of K-115, Y-27632, or HA-1077. PKACα (0.0625 ng/μL) is incubated at 25 °C for 30 min in 40 mmol/L Tris-HCl buffer (pH 7.5) containing 20 mmol/L MgCl₂, 1 mg/mL BSA, 5 μmol/L Kemptide peptide substrate, and 1 μmol/L ATP in a total volume of 40 μL. PKC (0.025 ng/μL) is incubated at 25 °C for 80 min in 20 mmol/L Tris-HCl buffer (pH 7.5) containing 20 mmol/L MgCl₂, 0.4 mmol/L CaCl₂, 0.1 mg/mL BSA, 0.25 mmol/L EGTA, 25 ng/mL phosphatidylserine, 2.5 ng/mL diacylglycerol, 0.0075% Triton-X-100, 25 μmol/L DTT, 10 μmol/L Neurogranin (28–43) peptide substrate, and 1 μmol/L ATP in a total volume of 40 μL. CaMKIIα (0.025 ng/μL) is incubated at 25 °C for 90 min in 50 mmol/L Tris-HCl buffer (pH 7.5) containing 10 mmol/L MgCl₂, 2 mmol/L CaCl₂, 0.04 mg/mL BSA, 16 μg/mL purified calmodulin from bovine testis, 500 μmol/L DTT, 50 μmol/L Autocamitide 2, and 1 μmol/L ATP in a total volume of 40 μL. After incubation, 40 μL of Kinase-Glo Luminescent Kinase Assay solution is added, and allowed to remain at 25 °C for 10 min, and Relative Light Units (RLU) are measured using a luminometer. The RLU without test compound is set as 100% (Control value), and that without enzyme and compound is set as 0% (Normal value). The reaction rate (% of control) is then calculated from the RLU with addition of each concentration of test compounds, and the 50% inhibitory concentrations (IC50) are determined by logistic regression analysis using SAS.
細胞アッセイ	細胞株	Cell-free assays
	濃度	IC50 of 51 and 19 nM for ROCK1 and ROCK2, respectively.
	反応時間
	実験の流れ
動物実験	動物モデル	Male C57BL/6 mice
	投薬量	1 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/24502505/
https://pubmed.ncbi.nlm.nih.gov/25277230/
https://pubmed.ncbi.nlm.nih.gov/26782355/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A human-specific RPGR isoform and a clinically approved Rho/ROCK inhibitor ameliorate defects associated with RPGR dysfunction [ Mol Ther Nucleic Acids, 2025, 36(4):102758]	PubMed: 41323795
Drug- and Cell-Type-Specific Effects of ROCK Inhibitors as a Potential Cause of Reticular Corneal Epithelial Edema [ Cells, 2025, 14(4)258]	PubMed: 39996731
Ponatinib and other clinically approved inhibitors of Src and Rho-A kinases abrogate dengue virus serotype 2- induced endothelial permeability [ Virulence, 2025, 16(1):2489751]	PubMed: 40189910
Drug and siRNA screens identify ROCK2 as a therapeutic target for ciliopathies [ Commun Med (Lond), 2025, 5(1):129]	PubMed: 40253509
Inhibitors of Rho kinases (ROCK) induce multiple mitotic defects and synthetic lethality in BRCA2-deficient cells [ Elife, 2023, 12e80254]	PubMed: 37073955
Characterization of mitotic phenotypes associated with a MYC synthetic lethal compound [ bioRxiv, 2023, 10.1101/2023.04.03.535438]	PubMed: None
Inhibition of Rho-associated protein kinase activity enhances oxidative phosphorylation to support corneal endothelial cell migration [ FASEB J, 2022, 36(7):e22397]	PubMed: 35661268
Lowering the Intraocular Pressure in Rats and Rabbits by Cordyceps cicadae Extract and Its Active Compounds [ Molecules, 2022, 27(3)707]	PubMed: 35163975
In situ immunogenic clearance induced by a combination of photodynamic therapy and rho-kinase inhibition sensitizes immune checkpoint blockade response to elicit systemic antitumor immunity against intraocular melanoma and its metastasis [ J Immunother Cancer, 2021, 9(1)e001481]	PubMed: 33479026
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19]	PubMed: 32645325

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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