Nitrovin hydrochloride
Based on 1 Customer Validation
Nitrovin (Difurazon) hydrochloride is an orally active inhibitor of thioredoxin reductase 1 (TrxR1) with both antibacterial and anticancer activities. Nitrovin hydrochloride induces ROS generation and endoplasmic reticulum stress by targeting and inhibiting TrxR1, which in turn induces cytoplasmic vacuolation, activates MAPK, and inhibits Alix. Nitrovin hydrochloride induces paraptosis-like non-apoptotic cell death, thereby exerting significant cytotoxicity against cancer cells. Nitrovin hydrochloride is used for research on glioblastoma, liver cancer, and bacterial infections.
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- Purity : 98.29%
- CAS No.: 2315-20-0
- 화학식: C14H13ClN6O6
- 분자량:396.74
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보관:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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
IC50 & Target
[1]|
TrxR1 |
In Vitro
Nitrovin (Difurazon) (1.25-10 µM; 24 h) hydrochloride inhibits cell viability in a concentration-dependent manner and exhibits significant cytotoxicity in 16 human tumor cell lines and 2 normal cell lines[1].
Nitrovin (1.25-10 µM; 24 h) hydrochloride decreases cell viability in a concentration-dependent manner, depletes intracellular ATP levels, and induces extensive characteristic cytoplasmic vacuolation in human glioblastoma U251 and U87 cells[1].
Nitrovin (0.625-5 µM; 24 h) hydrochloride downregulates the expression of the paraptosis-specific inhibitory protein Alix in a concentration-dependent manner in human glioblastoma U251 and U87 cells[1].
Nitrovin (1.25-5 µM; 4 h) hydrochloride concentration-dependently inhibits the catalytic activity of intracellular TrxR1 in human glioblastoma U251 and U87 cells[1].
Nitrovin (0.625-5 µM; 24 h) hydrochloride does not cause significant changes in Caspase-3 activity, does not induce cleavage activation of Caspase-3 and Caspase-7, does not cause typical apoptotic nuclear morphological changes such as nuclear condensation and nuclear fragmentation, and only induces a very low proportion of cells to be positive for Annexin V/7AAD apoptosis staining in human glioblastoma U251 cells[1].
Nitrovin (1.25-5 µM; 4 h) hydrochloride concentration-dependently induces significant accumulation of total intracellular ROS and a significant increase in mitochondrial superoxide levels in human glioblastoma U251 and U87 cells[1].
Nitrovin (5 µM; 2-24 h) hydrochloride induces cytoplasmic vacuolation and ROS generation and inhibits cell viability in human glioblastoma U251 cells transfected with control vector or overexpressing Alix, and Alix overexpression fails to reverse this cell death and does not alter ROS production levels[1].
Nitrovin (24 h) hydrochloride activates ARE/Nrf2 reporter gene transcription in human hepatocellular carcinoma HepG2 cells in a bell-shaped curve, activating ARE-bla signaling at low doses and causing cytotoxicity at high doses[5].
Nitrovin (5 µM; 24 h) hydrochloride induces significant large vacuole formation derived from endoplasmic reticulum swelling in human glioblastoma U251 and U87 cells[1].
Nitrovin (5 µM; 0.5-8 h) hydrochloride time-dependently upregulates the expression of endoplasmic reticulum stress marker proteins BiP, p-eIF2α, ATF4, and CHOP and rapidly induces ERK1/2 and p38 MAPK phosphorylation activation, followed by slightly later induction of JNK1/2 phosphorylation in human glioblastoma U251 cells[1].
Nitrovin (5 µM; 24 h) hydrochloride induces cytoplasmic vacuolation and death and induces ROS generation in human glioblastoma U251 cells transfected with control plasmid or overexpressing TrxR1; TrxR1 overexpression significantly inhibits vacuole accumulation and reverses cell death and significantly inhibits ROS generation[1].
Nitrovin (1-100 μg/mL; 2 days) hydrochloride inhibits most chicken cecal anaerobes at 100 μg/mL, whereas B. hypermegas (2 of 3 strains), Coprococcus sp. NE1/97, and Budding bacteria NE3/209 remain resistant[2].
Nitrovin (1 μg/dish; 12 h) hydrochloride induces significant frameshift mutations, base substitution mutations, and DNA cross-linking damage in Salmonella typhimurium TA97, TA100, and TA102, and triggers the formation of numerous His+ revertant colonies[6].
Nitrovin (0.625-5 µM; 0.5-24 h) hydrochloride does not alter the total expression level of TrxR1 protein in human glioblastoma U251 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U251 and U87 glioblastoma cells
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Concentration:1.25 µM、2.5 µM、5 µM、10 µM
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Incubation Time:24 h
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Result:Induced intracellular ROS formation in a concentration-dependent manner.
NAC or GSH pretreatment significantly reversed Nitrovin hydrochloride-induced ROS and cell death in both cell lines.
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Cell Line:U251 cells
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Concentration:0.625 µM, 1.25 µM, 2.5 µM, 5 µM
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Incubation Time:24 h
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Result:Produced no detectable cleavage of caspase-3 (pro-form 35 kDa; cleaved-forms 19/17 kDa) or caspase-7 (pro-form 35 kDa; cleaved-form 20 kDa).
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Cell Line:U251 cells
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Concentration:0.625 µM, 1.25 µM, 2.5 µM, 5 µM
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Incubation Time:24 h
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Result:Resulted in only a very minor percentage of Annexin V-positive apoptotic cells, confirming that cell death occurred predominantly via a non-apoptotic pathway.
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Cell Line:U251 and U87 cells
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Concentration:0.625 µM, 1.25 µM, 2.5 µM, 5 µM
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Incubation Time:24 h
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Result:Concentration-dependently downregulated the protein expression of Alix.
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Cell Line:U251 cells
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Concentration:0.625 µM, 1.25 µM, 2.5 µM, 5 µM
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Incubation Time:0.5, 1, 2, 4, 8, 24 h
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Result:Caused no statistically significant changes in total TrxR1 protein expression levels across different doses or time intervals.
In Vivo
Nitrovin (10 mg/kg; p.o.; free access; continuous administration) hydrochloride eliminates Gram-negative non-spore-forming anaerobes that constitute a major component of the cecal microbiota, while maintaining sufficient VFA concentrations and low pH to inhibit Salmonella typhimurium proliferation[2].
Nitrovin (10 mg/kg; p.o.; free access; continuous administration) hydrochloride significantly promotes the growth and development of neonatal healthy male Warren chicks in a 1-day-old rearing model, accompanied by a moderate increase in feed consumption and improved feed conversion ratio[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type larvae Zebrafish with Glioblastoma multiforme[1]
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Dosage:2.5 μM, 5 μM, 10 μM
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Administration:waterborne exposure; continuous immersion exposure starting at 2 days post-fertilization; 2 days of treatment/observation until 3 days post-microinjection
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Result:Reduced tumor fluorescence area to ~100% of control at 2.5 μM.
Reduced tumor fluorescence area to ~60% of control at 5 μM.
Reduced tumor fluorescence area to ~45% of control at 10 μM.
Showed inhibitory effect at 5 μM comparable to that of 100 μM TMZ.
Chemical Information
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CAS No. 2315-20-0
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Appearance Solid
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분자량 396.74
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화학식 C14H13ClN6O6
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Color Yellow to brown
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SMILES
O=[N+](C1=CC=C(/C=C/C(/C=C/C2=CC=C([N+]([O-])=O)O2)=N\NC(N)=N)O1)[O-].[H]Cl
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Synonyms
Difurazon hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
In Vitro:
DMSO : 5.83 mg/mL (14.69 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 (protect from light). 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 (protect from light). 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)
순도&문서
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Data Sheet (298 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhao L, et al. Nitrovin (difurazone), an antibacterial growth promoter, induces ROS-mediated paraptosis-like cell death by targeting thioredoxin reductase 1 (TrxR1). Biochemical pharmacology. 2023 Apr;210:115487. [Content Brief]
[3]. McCalla DR. Nitrofurans. InMechanism of action of antibacterial agents 1979 (pp. 176-213). Berlin.
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 (protect from light). 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 | 2.5205 mL | 12.6027 mL | 25.2054 mL | 63.0136 mL |
| 5 mM | 0.5041 mL | 2.5205 mL | 5.0411 mL | 12.6027 mL | |
| 10 mM | 0.2521 mL | 1.2603 mL | 2.5205 mL | 6.3014 mL |
Nitrovin hydrochloride Related Classifications
HY-129751 Related Classifications
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