SB-772077B dihydrochloride
Based on 1 Customer Validation
SB-772077B dihydrochloride is an orally active aminofuran-based Rho kinase ((ROCK)) inhibitor with IC50 values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytokines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases.
For research use only. We do not sell to patients.
- Purity: 99.33%
- CAS No.: 607373-46-6
- Formula: C15H20Cl2N8O2
- Molecular Weight:415.28
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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ROCK1 5.6 nM (IC50) |
ROCK2 6 nM (IC50) |
SB-772077-B dihydrochloride exhibits an IC50 value of 5.6 nM towards recombinant human ROCK1 and 6 nM towards human ROCK2[1].
SB-772077-B (3 μM; 30 min before Angiotensin II stimulation) dihydrochloride completely abolishes the Angiotensin II (HY-13948)-induced actin stress fiber formation in human primary aortic smooth muscle cells[1].
SB-772077-B (0.1-10 μM; 30 min before LPS) dihydrochloride dose-dependently reduces the production of LPS-induced inflammatory cytokines, including TNF-α and IL-6, in primary human macrophages[1].
SB-772077-B dihydrochloride induces profound dose-dependent relaxation of Phenylephrine (HY-B0769)-precontracted rat aortic rings with an IC50 of 39 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male spontaneously hypertensive rats (SHR), 8-10 weeks of age[1]
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Dosage:0.3 mg/kg, 1 mg/kg, 3 mg/kg
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Administration:Oral gavage
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Result:Showed the greatest effect on blood pressure approximately 2 hours after oral administration.
Caused an acute, dose-dependent increase in heart rate.
Chemical Information
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CAS No. 607373-46-6
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Appearance Solid
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Molecular Weight 415.28
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Formula C15H20Cl2N8O2
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Color White to off-white
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SMILES
[H]Cl.O=C(C1=CN=CC2=C1N(CC)C(C3=NON=C3N)=N2)N4C[C@@H](N)CC4.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 100 mg/mL (240.80 mM; Need ultrasonic)
DMSO : 38.33 mg/mL (92.30 mM; ultrasonic and warming and heat to 80°C; 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 3.83 mg/mL (9.22 mM); Clear solution
This protocol yields a clear solution of ≥ 3.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (38.3 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: ≥ 3.83 mg/mL (9.22 mM); Clear solution
This protocol yields a clear solution of ≥ 3.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (38.3 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 25 mg/mL (60.20 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (277 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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.4080 mL | 12.0401 mL | 24.0801 mL | 60.2003 mL |
| 5 mM | 0.4816 mL | 2.4080 mL | 4.8160 mL | 12.0401 mL | |
| 10 mM | 0.2408 mL | 1.2040 mL | 2.4080 mL | 6.0200 mL | |
| 15 mM | 0.1605 mL | 0.8027 mL | 1.6053 mL | 4.0134 mL | |
| 20 mM | 0.1204 mL | 0.6020 mL | 1.2040 mL | 3.0100 mL | |
| 25 mM | 0.0963 mL | 0.4816 mL | 0.9632 mL | 2.4080 mL | |
| 30 mM | 0.0803 mL | 0.4013 mL | 0.8027 mL | 2.0067 mL | |
| 40 mM | 0.0602 mL | 0.3010 mL | 0.6020 mL | 1.5050 mL | |
| 50 mM | 0.0482 mL | 0.2408 mL | 0.4816 mL | 1.2040 mL | |
| 60 mM | 0.0401 mL | 0.2007 mL | 0.4013 mL | 1.0033 mL | |
| 80 mM | 0.0301 mL | 0.1505 mL | 0.3010 mL | 0.7525 mL | |
| H2O | 100 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.6020 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
SB-772077B dihydrochloride Related Classifications
HY-108518 Related Classifications
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