Ripasudil free base
Based on 7 publication(s) in Google Scholar
Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
For research use only. We do not sell to patients.
- CAS No.: 223645-67-8
- Formula: C15H18FN3O2S
- Molecular Weight:323.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Ripasudil free base
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Adv Sci (Weinh). 2022 May;9(13):e2104682. [Abstract]
- Cancer Lett. 2026 Oct 1:657:218705.
- Mol Ther. 2023 Jun 7;31(6):1846-1856. [Abstract]
- Exp Eye Res. 2024 Aug:245:109977. [Abstract]
- Curr Eye Res. 2023 Sep;48(9):826-835. [Abstract]
- Preprints. 2023 May 15.
Customer Validation & Images
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In Vivo Imaging
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Cell Imaging/Staining
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WB
Biological Activity
Description
IC50 & Target
[1]|
ROCK2 19 nM (IC50) |
ROCK1 51 nM (IC50) |
CaMKIIa 370 nM (IC50) |
PKACa 2.1 μM (IC50) |
PKC 27 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A7R5 | EC50 |
210 nM
Compound: ripasudil
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Inhibition of ROCK-catalysed MLC Thr18/Ser19 phosphorylation in rat A7r5 cells after 90 mins by ELISA
Inhibition of ROCK-catalysed MLC Thr18/Ser19 phosphorylation in rat A7r5 cells after 90 mins by ELISA
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[PMID: 25898023] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 223645-67-8
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Molecular Weight 323.39
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Formula C15H18FN3O2S
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SMILES
FC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2
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Synonyms
K-115 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Adv Sci (Weinh)
Pharmacological Perturbation of Mechanical Contractility Enables Robust Transdifferentiation of Human Fibroblasts into Neurons. [Abstract]2022 May;9(13):e2104682. PMID: 35240008 -
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Mol Ther
ROCK inhibition enhanced hepatocyte liver engraftment by retaining membrane CD59 and attenuating complement activation. [Abstract]2023 Jun 7;31(6):1846-1856. PMID: 36860134
Ripasudil free base purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Jun 7;31(6):1846-1856. [Abstract]
C57 mice were transplanted with luciferase-expressing hepatocytes. The effects of the ROCK inhibitor Ripasudil (17.3 mg/kg, i.p.), nonmuscle myosin II ATPase inhibitor Blebbistatin, β1-integrin agonist Pyrintegrin, and Src kinase inhibitor Dasatinib on hepatocyte liver engraftment were analyzed by bioluminescence imaging on days 3 and 5 after intrasplenic infusion.
Ripasudil free base purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Jun 7;31(6):1846-1856. [Abstract]
Ripasudil (17.3 mg/kg, i.p.) treatment significantly decreased the colocalization between transplanted hepatocytes and Kupffer cells to 11.38% at 6 h and 14.49% at 12 h after transplantation.
Ripasudil free base purchased from MedChemExpress. Usage Cited in: Mol Ther. 2023 Jun 7;31(6):1846-1856. [Abstract]
Western blot assays showed rapid loss of CD59a protein on isolated hepatocytes, which could be blocked by Ripasudil (17.3 mg/kg, i.p.) treatment.
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Exp Eye Res
Laboratory exploration of the use of ripasudil in descemetorhexis with a human ex vivo model. [Abstract]2024 Aug:245:109977. PMID: 38901724 -
Curr Eye Res
Effects of Ripasudil, a Rho-Kinase Inhibitor, on Scar Formation in a Mouse Model of Filtration Surgery. [Abstract]2023 Sep;48(9):826-835. PMID: 37216470 -
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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