Fluparoxan
Based on 1 Customer Validation
Fluparoxan is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan is an anti-depressant agent.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 105182-45-4
- Formula: C10H10FNO2
- Molecular Weight:195.19
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Adrenergic Receptor Isoforms
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Biological Activity
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α2-adrenergic receptor |
In the rat isolated, field-stimulated vas deferens and the guinea-pig isolated, field-stimulated ileum preparations, Fluparoxan is a reversible competitive antagonist of the inhibitory responses to the alpha 2-adrenoceptor agonist UK-14304 (HY-B0659) with pKB values of 7.87 and 7.89 respectively[1].
In the rat isolated anococcygeus muscle, Fluparoxan is a much weaker competitive antagonist of the contractile response to the alpha 1-adrenoceptor agonist phenylephrine (HY-B0769) with a pKB of 4.45 giving an alpha 2: alpha 1-adrenoceptor selectivity ratio of greater than 2500[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fluparoxan (0.67-6 mg/kg, p.o.) prevents UK-14304 (HY-B0659)-induced sedation and bradycardia in the dog[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 105182-45-4
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Appearance Solid
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Molecular Weight 195.19
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Formula C10H10FNO2
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Color White to off-white
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SMILES
FC1=C2C(O[C@]3([H])[C@@](CNC3)([H])O2)=CC=C1
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Synonyms
GR50360
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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 : 50 mg/mL (256.16 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.81 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.
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 (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 5.1232 mL | 25.6161 mL | 51.2321 mL | 128.0803 mL |
| 5 mM | 1.0246 mL | 5.1232 mL | 10.2464 mL | 25.6161 mL | |
| 10 mM | 0.5123 mL | 2.5616 mL | 5.1232 mL | 12.8080 mL | |
| 15 mM | 0.3415 mL | 1.7077 mL | 3.4155 mL | 8.5387 mL | |
| 20 mM | 0.2562 mL | 1.2808 mL | 2.5616 mL | 6.4040 mL | |
| 25 mM | 0.2049 mL | 1.0246 mL | 2.0493 mL | 5.1232 mL | |
| 30 mM | 0.1708 mL | 0.8539 mL | 1.7077 mL | 4.2693 mL | |
| 40 mM | 0.1281 mL | 0.6404 mL | 1.2808 mL | 3.2020 mL | |
| 50 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5616 mL | |
| 60 mM | 0.0854 mL | 0.4269 mL | 0.8539 mL | 2.1347 mL | |
| 80 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6010 mL | |
| 100 mM | 0.0512 mL | 0.2562 mL | 0.5123 mL | 1.2808 mL |