Avizafone dihydrobromide
Based on 1 Customer Validation
Avizafone (Pro-diazepam) dihydrobromide, a pro-drug of Diazepam, is an anticonvulsant agent. Avizafone dihydrobromide can be used as an antidote of nerve agent poisoning. In vivo, Avizafone dihydrobromide is rapidly hydrolyzed by aminopeptidase to produce lysine and diazepam. Avizafone dihydrobromide has research areas including neurological disease, such as epilepsy.
For research use only. We do not sell to patients.
- CAS No.: 60067-15-4
- Formula: C22H29Br2ClN4O3
- Molecular Weight:592.75
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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)
Biological Activity
Description
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pigs (300-350 g)[2]
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Dosage:3.5 mg/kg
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Administration:i.m.; single dose
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Result:Reduced clinical sign severity to score 1 vs. 3 in controls, achieved 0% 24-hour mortality, prevented seizures in 0/8 animals, reduced necrosis to 3/8 animals vs. 4/4 in controls, eliminated perivascular cuffs and edema, prevented seizures in 0/8 animals vs. 4/8 with diazepam, eliminated brain lesions, and showed no significant respiratory parameter modifications.
Chemical Information
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CAS No. 60067-15-4
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Appearance Solid
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Molecular Weight 592.75
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Formula C22H29Br2ClN4O3
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SMILES
O=C(CNC([C@H](CCCCN)N)=O)N(C1=CC=C(C=C1C(C2=CC=CC=C2)=O)Cl)C.Br.Br
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Synonyms
Pro-diazepam dihydrobromide
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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
In Vitro:
DMSO : 100 mg/mL (168.71 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 (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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Clair P, et al. Stability study of a new antidote drug combination (Atropine-HI-6-Prodiazepam) for treatment of organophosphate poisoning. Eur J Pharm Sci. 2000 Jan;9(3):259-63. [Content Brief]
[2]. Lallement G, et al. Compared efficacy of diazepam or avizafone to prevent soman-induced electroencephalographic disturbances and neuropathology in primates: relationship to plasmatic benzodiazepine pharmacokinetics. Arch Toxicol. 2000 Oct;74(8):480-6. [Content Brief]
[3]. Taysse L, et al. Protection against soman-induced neuropathology and respiratory failure: a comparison of the efficacy of diazepam and avizafone in guinea pig. Toxicology. 2006;225(1):25-35. [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 (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 | 1 mM | 1.6871 mL | 8.4353 mL | 16.8705 mL | 42.1763 mL |
| 5 mM | 0.3374 mL | 1.6871 mL | 3.3741 mL | 8.4353 mL | |
| 10 mM | 0.1687 mL | 0.8435 mL | 1.6871 mL | 4.2176 mL | |
| 15 mM | 0.1125 mL | 0.5624 mL | 1.1247 mL | 2.8118 mL | |
| 20 mM | 0.0844 mL | 0.4218 mL | 0.8435 mL | 2.1088 mL | |
| 25 mM | 0.0675 mL | 0.3374 mL | 0.6748 mL | 1.6871 mL | |
| 30 mM | 0.0562 mL | 0.2812 mL | 0.5624 mL | 1.4059 mL | |
| 40 mM | 0.0422 mL | 0.2109 mL | 0.4218 mL | 1.0544 mL | |
| 50 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8435 mL | |
| 60 mM | 0.0281 mL | 0.1406 mL | 0.2812 mL | 0.7029 mL | |
| 80 mM | 0.0211 mL | 0.1054 mL | 0.2109 mL | 0.5272 mL | |
| 100 mM | 0.0169 mL | 0.0844 mL | 0.1687 mL | 0.4218 mL |