Rho-Kinase-IN-2
Based on 1 Customer Validation
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and CNS-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50 = 3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.
For research use only. We do not sell to patients.
- Purity: 98.80%
- CAS No.: 2573071-18-6
- Formula: C20H25FN4O2
- Molecular Weight:372.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
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Bioactive Compound Library
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Cell Cycle/DNA Damage Compound Library
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Immunology/Inflammation Compound Library
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Kinase Inhibitor Library
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Stem Cell Signaling Compound Library
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TGF-beta/Smad Compound Library
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Anti-Cancer Compound Library
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CNS-Penetrant Compound Library
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Anti-Aging Compound Library
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Reprogramming Compound Library
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Cytoskeleton Compound Library
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Orally Active Compound Library
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Anti-Pulmonary Fibrosis Compound Library
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Cancer Stem Cells Compound Library
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Heterocyclic Compound Library
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Highly Selective Inhibitors Library
HY-L158
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Serine/Threonine Kinase Inhibitor Library
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Extracellular Vesicles (EVs) Compound Library
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MCE Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Posttranslational Modification Library
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Biological Activity
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ROCK2 3 nM (IC50) |
Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A7r5 and PANC1 cells
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Concentration:0-10 mM
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Incubation Time:1 hour
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Result:Showed concentration-dependent effects, leading to an increase in AKT phosphorylation (EC50=28 nM) and a decrease in MYPT1 phosphorylation (IC50=14 nM).
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment[1].
Rho-Kinase-IN-2 (oral adiministration; 1-20 mg/kg; once) treatment shows a direct dose- and time-dependent relationship between brain exposure and MYPT1 phosphorylation status[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; once) treatment decreases in the mean arterial, systolic, diastolic blood pressure, and heart rate[1].
Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice[1]
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Dosage:10 mg/kg
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Administration:Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h
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Result:Observed dose- and time-dependent ROCK1 and ROCK2 TE, with a free brain KiNativ ROCK1 and ROCK2 IC50=∼6 nM.
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Animal Model:3−4 months old heterozygote Q175DN KI and wild-type littermate mice[1]
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Dosage:10 or 20 mg/kg
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Administration:Oral adiministration; 10 or 20 mg/kg; once a day or twice a day; 2 weeks
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Result:Scored neurological index normally at all doses although a slight loss in bodyweight (∼2%) in the 20 mg/kg treatment group.
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Animal Model:Heterozygote HTT zQ175DN knock-in mice[1]
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Dosage:1-20 mg/kg
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Administration:Oral adiministration; 1-20 mg/kg; once
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Result:Remained over MYPT1 IC50 for over 2 h of the free brain at 10 mg/kg, and observed the dose- and time-dependent inhibition of MYPT1 phosphorylation in the striatum following acute in vivo dosing.
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Animal Model:CD1 mice[1]
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Dosage:10 and 20 mg/kg
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Administration:Oral adiministration; 10 or 20 mg/kg; once
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Result:Observed the decreases in the mean arterial (maximum change of 61.0 ± 8.5 mmHg from baseline), systolic (maximum change of 59.5 ± 8.4 mmHg from baseline), diastolic blood pressure (maximum change of 56.4 ± 9.0 mmHg from baseline), and heart rate (maximum change from predose of 107 bpm) when compared to the control group from ∼0.5 to 2 h post dose.
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Animal Model:Heterozygote Q175DN KI mouse model of HD[1]
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Dosage:10 mg/kg
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Administration:Oral adiministration; 10 mg/kg; twice a day; 90 days
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Result:Led to lower-than-expected brain concentrations compared to single dosing.
Chemical Information
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CAS No. 2573071-18-6
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Appearance Solid
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Molecular Weight 372.44
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Formula C20H25FN4O2
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Color Light yellow to yellow
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SMILES
O=C(N1[C@H](C)CN(C2=C(F)C=NC=C2)CC1)N[C@@H](C3=CC=CC(OC)=C3)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (134.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6850 mL | 13.4250 mL | 26.8500 mL | 67.1249 mL |
| 5 mM | 0.5370 mL | 2.6850 mL | 5.3700 mL | 13.4250 mL | |
| 10 mM | 0.2685 mL | 1.3425 mL | 2.6850 mL | 6.7125 mL | |
| 15 mM | 0.1790 mL | 0.8950 mL | 1.7900 mL | 4.4750 mL | |
| 20 mM | 0.1342 mL | 0.6712 mL | 1.3425 mL | 3.3562 mL | |
| 25 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6850 mL | |
| 30 mM | 0.0895 mL | 0.4475 mL | 0.8950 mL | 2.2375 mL | |
| 40 mM | 0.0671 mL | 0.3356 mL | 0.6712 mL | 1.6781 mL | |
| 50 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 60 mM | 0.0447 mL | 0.2237 mL | 0.4475 mL | 1.1187 mL | |
| 80 mM | 0.0336 mL | 0.1678 mL | 0.3356 mL | 0.8391 mL | |
| 100 mM | 0.0268 mL | 0.1342 mL | 0.2685 mL | 0.6712 mL |
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