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Chemical Structure| 887375-67-9 Chemical Structure| 887375-67-9

Structure of Ripasudil
CAS No.: 887375-67-9

Chemical Structure| 887375-67-9

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K-115 HCl is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

Synonyms: K-115; K-115 Hydrochloride Dihydrate; Ripasudil hydrochloride dihydrate

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Product Details of Ripasudil

CAS No. :887375-67-9
Formula : C15H23ClFN3O4S
M.W : 395.88
SMILES Code : O=S(C1=CC=CC2=C1C(F)=CN=C2)(N3[C@@H](C)CNCCC3)=O.[H]O[H].[H]O[H].[H]Cl
Synonyms :
K-115; K-115 Hydrochloride Dihydrate; Ripasudil hydrochloride dihydrate
MDL No. :MFCD26960897
InChI Key :CMDJNMACGABCKQ-XVSRHIFFSA-N
Pubchem ID :11625386

Safety of Ripasudil

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ripasudil

cytoskeleton

Isoform Comparison

Biological Activity

Target
  • ROCK1

    ROCK1, IC50:51 nM

  • ROCK2

    ROCK2, IC50:19 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
FECD corneal endothelial cells (SVF1-73F, SVF3-76M, SVF5-54F) 1 µM 24 h To evaluate the effect of Ripasudil on FECD cell migration and wound healing, results showed that Ripasudil significantly enhanced FECD cell migration speed and wound healing ability. Cells. 2024 Jul 19;13(14):1218.
Normal corneal endothelial cells (SVN1-67F) 1 µM 24 h To evaluate the effect of Ripasudil on cell migration and wound healing, results showed that Ripasudil significantly enhanced cell migration speed and wound healing ability. Cells. 2024 Jul 19;13(14):1218.
A10 VSMCs 0.1 μM 30 min Ripasudil partially blocked the effect of MYDGF on maintaining the differentiated phenotype of A10 VSMCs, indicating that Ripasudil affected MYDGF's role by inhibiting the ROCK signaling pathway. Acta Pharmacol Sin. 2024 Jan;45(1):98-111.
Hepatocytes 4 µM 1 hour Ripasudil protects hepatocytes by inhibiting complement activation and blocking the formation of the membrane attack complex, thereby enhancing hepatocyte survival and engraftment. Mol Ther. 2023 Jun 7;31(6):1846-1856.
Primary human corneal epithelial cells (pHCEpCs) 10 µM and 30 µM 7 days To investigate the effects of Ripasudil on the barrier function of human corneal epithelial cells, the results showed that Ripasudil upregulated the expression of tight and adherens junction-related genes, improving epithelial barrier function. Cells. 2025 Feb 11;14(4):258.
Primary human corneal endothelial cells (pHCEnCs) 10 µM and 30 µM 72 h To investigate the effects of Ripasudil on the proliferation and migration of human corneal endothelial cells, the results showed that Ripasudil significantly increased cell proliferation and migration. Cells. 2025 Feb 11;14(4):258.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice C57BL/6 mice Intraperitoneal injection 17.3 mg/kg Once daily for 3 days Ripasudil significantly enhanced hepatocyte engraftment and accelerated liver repopulation by inhibiting complement activation and Kupffer cell phagocytosis. Mol Ther. 2023 Jun 7;31(6):1846-1856.
Mice Acute liver injury model Intraperitoneal injection 50 mg/kg Single dose, 5 hours duration Ripasudil enhanced NEMO expression by inhibiting ROCK1 and ameliorated APAP-induced liver injury. Theranostics. 2024 Feb 24;14(5):1841-1859
Mice Acute liver injury model Intraperitoneal injection 50 mg/kg Single dose, lasting 5 hours Ripasudil significantly inhibited APAP-induced acute liver injury, reduced lipid peroxidation, suppressed ALOX12 expression, and increased GPX4 levels. Theranostics. 2022 Jan 9;12(4):1570-1588

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.63mL

2.53mL

1.26mL

25.26mL

5.05mL

2.53mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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