Antazoline hydrochloride
Based on 1 Customer Validation
Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV.
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- Pureza: 99.60%
- No. CAS: 2508-72-7
- Fòrmula: C17H20ClN3
- Peso molecular:301.81
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
Descripciòn
In Vitro
Antazoline hydrochloride (10-100 μmol/L, 72 h) exhibits dose-dependent inhibition of HBV DNA and no significant cytotoxicity in HepAD38 cells[2].
Antazoline hydrochloride (100 μmol/L, 5 d) has inhibitory effect against HBV DNA (EC50 = 2.91 μmol/L) in HepAD38 cells[2].
Antazoline hydrochloride (0.123-30 μmol/L, 96 h) has a significant inhibitory effect on HBV DNA in Huh7 cells (EC50 = 2.349 μmol/L)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | CL | Vd |
|---|---|---|---|---|---|---|---|---|---|
| Rat | 10 mg/kg | i.v. | 3.53 h | 2.755 mg·h/L | 3.238 mg·h/L | 1.99 h | 3.67 h | 3.1 L/h/kg | 15.7 L/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2508-72-7
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Appearance Solid
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Peso molecular 301.81
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Fòrmula C17H20ClN3
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Color White to off-white
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SMILES
[H]Cl.C1(CN(C2=CC=CC=C2)CC3=CC=CC=C3)=NCCN1
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Synonyms
Phenazoline hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (82.83 mM; ultrasonic and warming and heat to 60°C; 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)
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 (8.28 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.28 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. 1. Wang, R., et al., (2013). Determination of antazoline hydrochloride in rat plasma and excreta by reversed-phase ion-pair chromatography and its application to pharmacokinetics. Biomedical chromatography : BMC, 27(12), 1595–1602. [Content Brief]
[2]. Li, J., et al., (2021). Repurposing of Antazoline Hydrochloride as an Inhibitor of Hepatitis B Virus DNA Secretion. Virologica Sinica, 36(3), 501–509. [Content Brief]
[3]. Gehring, D. A., & Kehler, J. G. (1970). Conversion of atrial fibrillation with antazoline hydrochloride (Arithmin). Angiology, 21(1), 11–17. [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 | 3.3133 mL | 16.5667 mL | 33.1334 mL | 82.8336 mL |
| 5 mM | 0.6627 mL | 3.3133 mL | 6.6267 mL | 16.5667 mL | |
| 10 mM | 0.3313 mL | 1.6567 mL | 3.3133 mL | 8.2834 mL | |
| 15 mM | 0.2209 mL | 1.1044 mL | 2.2089 mL | 5.5222 mL | |
| 20 mM | 0.1657 mL | 0.8283 mL | 1.6567 mL | 4.1417 mL | |
| 25 mM | 0.1325 mL | 0.6627 mL | 1.3253 mL | 3.3133 mL | |
| 30 mM | 0.1104 mL | 0.5522 mL | 1.1044 mL | 2.7611 mL | |
| 40 mM | 0.0828 mL | 0.4142 mL | 0.8283 mL | 2.0708 mL | |
| 50 mM | 0.0663 mL | 0.3313 mL | 0.6627 mL | 1.6567 mL | |
| 60 mM | 0.0552 mL | 0.2761 mL | 0.5522 mL | 1.3806 mL | |
| 80 mM | 0.0414 mL | 0.2071 mL | 0.4142 mL | 1.0354 mL |
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