Azalanstat
Based on 1 Customer Validation
Azalanstat (RS-21607) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats.
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- Reinheit: 99.52%
- CAS. Nr.: 143393-27-5
- Formel: C22H24ClN3O2S
- Molecular Weight:429.96
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Azalanstat (Compound I) inhibits rat spleen microsomal HO-1 (IC50 = 5.8 μM) and rat brain microsomal HO-2 (IC50 = 28.0 μM) in vitro, with a selectivity index of 5 for HO-1 over HO-2[1].
Azalanstat (0-100 μM) inhibits the activity of rat liver microsomal CYP3A1/3A2 in vitro, with an IC50 of 48.1 μM[1].
Azalanstat (0-200 μM; 3-24 h, or 6 h + 24 h inhibitor-free culture) reduces GVBD in a dose- and time-dependent manner at high concentrations (≥50 μM for 6 h treatment, ≥10 μM for 24 h treatment), while increasing the degree of oocyte degeneration; notably, oocyte degeneration becomes irreversible after 6 h of treatment at 100 μM[2].
Azalanstat (1-100 μM; 6-24 h with 5 μg/mL LH) reduces LH-induced GVBD in a dose-dependent manner, accompanied by increased degeneration of oocytes and follicles at 1-100 μM with a 24 h treatment[2].
Azalanstat (1-100 μM; 6-24 h with 5 μg/mL LH) partially inhibits LH-induced progesterone synthesis in preovulatory rat follicles in vitro in a dose-dependent manner when applied at concentrations of 1, 50, and 100 μM for 6 or 24 h[2].
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:Wistar-derived rats (female, 23-24 days of age, injected with 10 IU eCG then 4 IU hCG to induce ovulatory dysfunction model)[2]
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Dosage:2.15-215 μg/bursa
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Administration:intrabursal injection; single dose
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Result:Caused statistically significant inhibition of ovulation.
Chemical Information
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CAS. Nr. 143393-27-5
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Appearance Solid
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Molecular Weight 429.96
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Formel C22H24ClN3O2S
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Color White to off-white
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SMILES
ClC(C=C1)=CC=C1CC[C@]2(O[C@@H](CO2)CSC3=CC=C(C=C3)N)CN4C=CN=C4
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Synonyms
RS-21607
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (232.58 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.3258 mL | 11.6290 mL | 23.2580 mL | 58.1449 mL |
| 5 mM | 0.4652 mL | 2.3258 mL | 4.6516 mL | 11.6290 mL | |
| 10 mM | 0.2326 mL | 1.1629 mL | 2.3258 mL | 5.8145 mL | |
| 15 mM | 0.1551 mL | 0.7753 mL | 1.5505 mL | 3.8763 mL | |
| 20 mM | 0.1163 mL | 0.5814 mL | 1.1629 mL | 2.9072 mL | |
| 25 mM | 0.0930 mL | 0.4652 mL | 0.9303 mL | 2.3258 mL | |
| 30 mM | 0.0775 mL | 0.3876 mL | 0.7753 mL | 1.9382 mL | |
| 40 mM | 0.0581 mL | 0.2907 mL | 0.5814 mL | 1.4536 mL | |
| 50 mM | 0.0465 mL | 0.2326 mL | 0.4652 mL | 1.1629 mL | |
| 60 mM | 0.0388 mL | 0.1938 mL | 0.3876 mL | 0.9691 mL | |
| 80 mM | 0.0291 mL | 0.1454 mL | 0.2907 mL | 0.7268 mL | |
| 100 mM | 0.0233 mL | 0.1163 mL | 0.2326 mL | 0.5814 mL |
Azalanstat Related Classifications
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