| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cotosudil selectively inhibits Rho-associated protein kinase 1 (ROCK1), a key regulator of the actin cytoskeleton. ROCK1 is involved in various cellular processes including smooth muscle contraction, cell migration, proliferation, and apoptosis. Inhibition of ROCK1 leads to relaxation of the trabecular meshwork and increased aqueous humor outflow, reducing intraocular pressure in glaucoma. The compound also has potential applications in cardiovascular and neurodegenerative diseases through modulation of ROCK-mediated signaling pathways.
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| ln Vitro |
Cotosudil demonstrates in vitro activity as a ROCK kinase inhibitor. It has anti-hypertensive activity in vitro. The compound's inhibition of ROCK1 leads to downstream effects on the actin cytoskeleton and cellular contractility. As a ROCK inhibitor, it shows potential for modulating various cellular processes involved in disease pathology. Detailed in vitro potency data (IC50 values) and selectivity profiles are available in the primary literature and compound documentation.
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| ln Vivo |
Cotosudil has demonstrated efficacy and tolerability in preclinical and early clinical studies. It can be used for glaucoma or ocular hypertension research in animal models. As a ROCK kinase inhibitor, it has anti-hypertensive activity. The compound's efficacy in reducing intraocular pressure has been demonstrated in preclinical studies, supporting its development as a topical agent for glaucoma treatment. Further clinical studies are ongoing to evaluate its safety and efficacy in patients.
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| Enzyme Assay |
For ROCK1 kinase inhibition assays, purified ROCK1 enzyme is incubated with ATP and a peptide substrate in the presence of Cotosudil at various concentrations. Kinase activity is measured by quantifying phosphorylation of the substrate using radiometric (33P-ATP incorporation) or fluorescence-based (time-resolved FRET) methods. IC50 values are calculated from dose-response curves. Selectivity profiling is conducted by screening the compound against a panel of related kinases to assess specificity for ROCK1 versus other kinases.
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| Cell Assay |
For cellular activity studies, relevant cell types (e.g., trabecular meshwork cells, smooth muscle cells) are cultured in appropriate media. Cells are treated with Cotosudil at various concentrations for 24-72 hours. ROCK1 inhibition is assessed by measuring phosphorylation of downstream targets such as myosin light chain (MLC) or LIM kinase by Western blot. Cell morphology and actin cytoskeleton organization are evaluated by phalloidin staining and fluorescence microscopy. Cell proliferation is assessed by MTT or BrdU incorporation assays, and apoptosis is measured by caspase-3/7 activity or Annexin V staining.
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| Animal Protocol |
For in vivo efficacy studies, animal models of glaucoma or ocular hypertension are used. Cotosudil is administered topically as eye drops or by other appropriate routes at various doses. Intraocular pressure is measured using a tonometer at baseline and at various time points after treatment. For cardiovascular studies, appropriate animal models are used to assess blood pressure reduction and vascular function. For neurodegenerative studies, relevant disease models are employed to evaluate neuroprotective effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cotosudil have been characterized in preclinical studies. As a ROCK inhibitor intended for topical ocular administration, the compound is designed to achieve therapeutic concentrations in the eye with minimal systemic exposure. The compound's pharmacokinetic profile supports its development as a topical agent for glaucoma treatment. Detailed PK parameters including ocular bioavailability, half-life, and systemic exposure are available in the primary literature. The compound is typically formulated as eye drops for topical administration.
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| Toxicity/Toxicokinetics |
Cotosudil has demonstrated efficacy and tolerability in preclinical and early clinical studies. As a ROCK kinase inhibitor, it has anti-hypertensive activity and can be used for glaucoma or ocular hypertension research. The compound is also being investigated for potential applications in cataracts, cardiovascular diseases, and neurodegenerative diseases. Comprehensive toxicological studies have been conducted as part of preclinical development. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
Cotosudil is a selective ROCK1 inhibitor developed for glaucoma and ocular hypertension treatment, with molecular formula not specified in available sources. It has anti-hypertensive activity and potential applications in cataracts, cardiovascular diseases, and neurodegenerative diseases. The compound has demonstrated efficacy and tolerability in preclinical and early clinical studies. Cotosudil is for research use only and has not been approved for clinical applications. It is primarily used in glaucoma and ocular hypertension research.
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| Molecular Formula |
C16H21N3O2S
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|---|---|
| Molecular Weight |
319.421842336655
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| Exact Mass |
319.135
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| CAS # |
1258833-31-6
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| Related CAS # |
1258833-31-6;1258832-72-2 (2HCl);
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| PubChem CID |
49847659
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| Appearance |
White to off-white solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
463
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S(C1C=CC2C=NC=CC=2C=1)(N1CCCCNC[C@H]1C)(=O)=O
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| InChi Key |
OIJDBECSPSHUGA-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C16H21N3O2S/c1-13-11-17-7-2-3-9-19(13)22(20,21)16-5-4-15-12-18-8-6-14(15)10-16/h4-6,8,10,12-13,17H,2-3,7,9,11H2,1H3/t13-/m1/s1
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| Chemical Name |
6-[[(2R)-2-methyl-1,4-diazocan-1-yl]sulfonyl]isoquinoline
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| HS Tariff Code |
2934.99.9001
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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) |
DMSO : 50 mg/mL (156.53 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.83 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 25.0 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: ≥ 2.5 mg/mL (7.83 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 25.0 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: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1307 mL | 15.6534 mL | 31.3067 mL | |
| 5 mM | 0.6261 mL | 3.1307 mL | 6.2613 mL | |
| 10 mM | 0.3131 mL | 1.5653 mL | 3.1307 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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