Vicadrostat
Based on 1 Customer Validation
Vicadrostat (BI 690517) is an orally active aldosterone synthase (aldosterone synthase) inhibitor, with IC50 values of 19 nM, 16 nM, and 18 μM against human, cynomolgus monkey, and rat aldosterone synthase, respectively. Vicadrostat has an in vivo IC50 of 25 nM for aldosterone synthesis. Vicadrostat exhibits high selectivity for cortisol synthase; it reduces aldosterone production and decreases plasma aldosterone levels. Vicadrostat can be used in the research of chronic kidney disease, heart failure, and hypertension.
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- Purity : 98.67%
- CAS No.: 1868065-21-7
- 화학식: C15H12ClN3O3
- 분자량:317.73
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보관:Powder -20°C, 3 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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Macaca fascicularis (male, 4-7 years, 4.2-5.9 kg, 5-day repeat dosing model)[1]
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Dosage:0.05 mg/kg (twice daily); 0.1 mg/kg (twice daily; once daily)
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Administration:p.o.; twice daily for 5 days; once daily for 5 days
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Result:Maintained long-term and effective aldosterone reduction with better tolerance when administered in a partial-time manner (once daily).
Triggered unknown but powerful counter-regulatory mechanisms, resulting in compensatory rebound of aldosterone levels in the later stages of treatment, thereby nullifying the therapeutic effect at continuous suppression throughout the day (twice daily).
Chemical Information
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CAS No. 1868065-21-7
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Appearance Solid
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분자량 317.73
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화학식 C15H12ClN3O3
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Color White to off-white
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SMILES
O=C1C2=C(C[C@@](C)(O1)CO)N=CN2C3=CC(Cl)=C(C=C3)C#N
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Synonyms
BI 690517
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (314.73 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)
In Vivo:
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: ≥ 2.5 mg/mL (7.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
순도&문서
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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. 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 | 1 mM | 3.1473 mL | 15.7366 mL | 31.4733 mL | 78.6832 mL |
| 5 mM | 0.6295 mL | 3.1473 mL | 6.2947 mL | 15.7366 mL | |
| 10 mM | 0.3147 mL | 1.5737 mL | 3.1473 mL | 7.8683 mL | |
| 15 mM | 0.2098 mL | 1.0491 mL | 2.0982 mL | 5.2455 mL | |
| 20 mM | 0.1574 mL | 0.7868 mL | 1.5737 mL | 3.9342 mL | |
| 25 mM | 0.1259 mL | 0.6295 mL | 1.2589 mL | 3.1473 mL | |
| 30 mM | 0.1049 mL | 0.5246 mL | 1.0491 mL | 2.6228 mL | |
| 40 mM | 0.0787 mL | 0.3934 mL | 0.7868 mL | 1.9671 mL | |
| 50 mM | 0.0629 mL | 0.3147 mL | 0.6295 mL | 1.5737 mL | |
| 60 mM | 0.0525 mL | 0.2623 mL | 0.5246 mL | 1.3114 mL | |
| 80 mM | 0.0393 mL | 0.1967 mL | 0.3934 mL | 0.9835 mL | |
| 100 mM | 0.0315 mL | 0.1574 mL | 0.3147 mL | 0.7868 mL |
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