Oxolamine citrate
Based on 1 Customer Validation
Oxolamine citrate (SKF-9976 citrate) is an orally active antitussive. Oxolamine citrate can inhibit CYP2B1/2. Oxolamine citrate has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine citrate increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine citrate can be used in respiratory disease research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.87%
- CAS. Nr.: 1949-20-8
- Formel: C20H27N3O8
- Molecular Weight:437.44
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Speicherung:
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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Biologische Aktivität
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CYP2B1 |
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Oxolamine (10 μg/mL; 24 h) citrate significantly reduces the plasma protein binding of Clarithromycin (HY-17508) in fresh rat plasma[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Oxolamine citrate (80 mg/kg body weight initially, then 53.3 mg/kg; i.p.; 11 times at 3, 6, 9, 24, 28, 32, 48, 52, 56, 72 and 76 h) shows a distinct anti-inflammatory action on the respiratory organs of guinea pigs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pigs + non-bacterial inflammation of the respiratory tract model induced by inhalation of acrolein aerosol[4]
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Dosage:80 mg/kg body weight initially, then 53.3 mg/kg
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Administration:Intraperitoneal injection, 11 times at 3, 6, 9, 24, 28, 32, 48, 52, 56, 72 and 76 h
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Result:Reduced relative lung weight.
Significantly reduced inflammation levels.
Protected the pulmonary parenchyma from emphysema.
Showed anti-inflammatory effect superior to that of Phenylbutyrone.
Chemical Information
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CAS. Nr. 1949-20-8
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Appearance Solid
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Molecular Weight 437.44
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Formel C20H27N3O8
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Color White to off-white
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SMILES
CCN(CC)CCC1=NC(C2=CC=CC=C2)=NO1.O=C(CC(C(O)=O)(O)CC(O)=O)O
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Synonyms
SKF-9976 citrate; AF-438 citrate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (228.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 14.29 mg/mL (32.67 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.72 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 (5.72 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 28 mg/mL (64.01 mM); Clear solution; Need ultrasonic
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.
Reinheit & Dokumentation
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Data Sheet (281 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)
Verweise
[1]. Kirilmaz L, et, al. Sustained-release dosage form of oxolamine citrate: preparation and release kinetics. J Microencapsul. Apr-Jun 1992;9(2):167-72. [Content Brief]
[2]. GIUDICI G, et, al. [On the anti-inflammatory action of oxolamine citrate]. Minerva Med. 1961 Oct 31;52:3752-5. [Content Brief]
[3]. Zhu X, et al. Gender difference in the pharmacokinetic interaction between oral warfarin and oxolamine in rats: inhibition of CYP2B1 by oxolamine in male rats. Biopharm Drug Dispos. 2007 Apr;28(3):125-33. [Content Brief]
[4]. Dahlgren S, et al. The effect of oxolamine citrate on experimentally produced inflammation in the respiratory organs. Acta Pharmacol Toxicol (Copenh). 1966;24(2):286-96. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2860 mL | 11.4301 mL | 22.8603 mL | 57.1507 mL |
| 5 mM | 0.4572 mL | 2.2860 mL | 4.5721 mL | 11.4301 mL | |
| 10 mM | 0.2286 mL | 1.1430 mL | 2.2860 mL | 5.7151 mL | |
| 15 mM | 0.1524 mL | 0.7620 mL | 1.5240 mL | 3.8100 mL | |
| 20 mM | 0.1143 mL | 0.5715 mL | 1.1430 mL | 2.8575 mL | |
| 25 mM | 0.0914 mL | 0.4572 mL | 0.9144 mL | 2.2860 mL | |
| 30 mM | 0.0762 mL | 0.3810 mL | 0.7620 mL | 1.9050 mL | |
| DMSO | 40 mM | 0.0572 mL | 0.2858 mL | 0.5715 mL | 1.4288 mL |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4572 mL | 1.1430 mL | |
| 60 mM | 0.0381 mL | 0.1905 mL | 0.3810 mL | 0.9525 mL | |
| 80 mM | 0.0286 mL | 0.1429 mL | 0.2858 mL | 0.7144 mL | |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5715 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Oxolamine citrate Related Classifications
HY-B1042 Related Classifications
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