Nitrefazole
Based on 1 Customer Validation
Nitrefazole (EMD-15700) is an aldehyde dehydrogenase (ALDH) inhibitor. Nitrefazole specifically inhibits human liver ALDH I and human erythrocyte ALDH isozymes, but does not alter the activity of human liver ALDH II or human placental ALDH. Nitrefazole effectively promotes exosome secretion in prostate cancer cells by increasing the levels of Alix, nSMase2, Rab27a and p-ERK. Nitrefazole can be used in studies related to prostate cancer.
For research use only. We do not sell to patients.
- Purity: 99.44%
- CAS No.: 21721-92-6
- Formula: C10H8N4O4
- Molecular Weight:248.19
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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ALDH1 |
Nitrefazole (20 µM) increases exosome production from human prostate cancer C4-2B cells by upregulating Rab27a, Alix, nSMase2, and p-ERK levels[2].
Nitrefazole (100 μM) significantly inhibits human hepatic ALDH II (90% inhibition) and erythrocyte high-Km ALDH (37% inhibition) at pH 7.4, significantly inhibits human hepatic ALDH I (32% inhibition) at pH 8.8, inhibits human hepatic ALDH I (26% inhibition) and erythrocyte low-Km ALDH (35% inhibition) at pH 7.4, and does not significantly inhibit human hepatic ALDH II at pH 8.8 or human placental ALDH at pH 8.8[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 21721-92-6
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Appearance Solid
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Molecular Weight 248.19
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Formula C10H8N4O4
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Color White to off-white
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SMILES
CC1=NC([N+]([O-])=O)=CN1C2=CC=C([N+]([O-])=O)C=C2
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Synonyms
EMD-15700
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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 : 100 mg/mL (402.92 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: ≥ 2.5 mg/mL (10.07 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.
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 (274 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)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Datta A, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Scientific reports. 2018 May 25;8(1):8161. [Content Brief]
[2]. Joo HS, et al. Current Knowledge and Future Perspectives on Mesenchymal Stem Cell-Derived Exosomes as a New Therapeutic Agent. International journal of molecular sciences. 2020 Jan 22;21(3):727. [Content Brief]
[3]. Zorzano A, et al. Differences in the kinetic properties and sensitivity to inhibitors of human placental, erythrocyte, and major hepatic aldehyde dehydrogenase isoenzymes. Biochemical pharmacology. 1990 Mar 01;39(5):873-8. [Content Brief]
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 | 4.0292 mL | 20.1459 mL | 40.2917 mL | 100.7293 mL |
| 5 mM | 0.8058 mL | 4.0292 mL | 8.0583 mL | 20.1459 mL | |
| 10 mM | 0.4029 mL | 2.0146 mL | 4.0292 mL | 10.0729 mL | |
| 15 mM | 0.2686 mL | 1.3431 mL | 2.6861 mL | 6.7153 mL | |
| 20 mM | 0.2015 mL | 1.0073 mL | 2.0146 mL | 5.0365 mL | |
| 25 mM | 0.1612 mL | 0.8058 mL | 1.6117 mL | 4.0292 mL | |
| 30 mM | 0.1343 mL | 0.6715 mL | 1.3431 mL | 3.3576 mL | |
| 40 mM | 0.1007 mL | 0.5036 mL | 1.0073 mL | 2.5182 mL | |
| 50 mM | 0.0806 mL | 0.4029 mL | 0.8058 mL | 2.0146 mL | |
| 60 mM | 0.0672 mL | 0.3358 mL | 0.6715 mL | 1.6788 mL | |
| 80 mM | 0.0504 mL | 0.2518 mL | 0.5036 mL | 1.2591 mL | |
| 100 mM | 0.0403 mL | 0.2015 mL | 0.4029 mL | 1.0073 mL |