Fenspiride hydrochloride
Based on 1 Customer Validation
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 5053-08-7
- Formula: C15H21ClN2O2
- Molecular Weight:296.79
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
PDE3 |
PDE4 |
PDE5 |
Fenspiride (around 100 μM) inhibits histamine-induced contraction of isolated guinea pig trachea[2].
Fenspiride (≤1000 μM) produces less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages[3].
Fenspiride (60 mg/kg; p.o. for 3 days) reduces the increased serum concentrations of extracellular type II phospholipase A 2, the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lipopolysaccharide-treated Male Dunkin-Hartley guinea-pigs weighing 400-600 g[3]
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Dosage:60 mg/kg
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Administration:Orally for 3 days; pretreated
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Result:Reduced the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum (4.2 vs. 2.3 ng/ml) and in the BALF (55.7 vs. 19.7 ng/ml).
Reduced the lipopolysaccharide-induced primed stimulation of alveolar macrophages, (1551.5 vs 771.5 pg/μg protein, P<0.05 for thromboxane B2 and 12.6 vs. 3.6 pg/μg protein, P<0.05 for leukotriene C4).
Reduced the increased serum concentrations of extracellular type II phospholipase A 2 (3.9 vs. 1.2 nmol/ml per min), the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide.
Chemical Information
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CAS No. 5053-08-7
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Appearance Solid
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Molecular Weight 296.79
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Formula C15H21ClN2O2
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Color White to off-white
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SMILES
O=C1OC2(CCN(CCC3=CC=CC=C3)CC2)CN1.Cl
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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
H2O : 50 mg/mL (168.47 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (112.30 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.
* 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.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (9.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (9.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: 120 mg/mL (404.33 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (274 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]. Matuszewska A, et al. Long-term administration of fenspiride has no negative impact on bone mineral density and bone turnover in young growing rats. Adv Clin Exp Med. 2019 Jun;28(6):771-776. [Content Brief]
[2]. Cortijo J, et al. Effects of fenspiride on human bronchial cyclic nucleotide phosphodiesterase isoenzymes: functional and biochemical study. Eur J Pharmacol. 1998 Jan 2;341(1):79-86. [Content Brief]
[3]. De Castro CM, et al. Fenspiride: an anti-inflammatory drug with potential benefits in the treatment of endotoxemia. Eur J Pharmacol. 1995 Dec 29;294(2-3):669-76. [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 / H2O | 1 mM | 3.3694 mL | 16.8469 mL | 33.6939 mL | 84.2346 mL |
| 5 mM | 0.6739 mL | 3.3694 mL | 6.7388 mL | 16.8469 mL | |
| 10 mM | 0.3369 mL | 1.6847 mL | 3.3694 mL | 8.4235 mL | |
| 15 mM | 0.2246 mL | 1.1231 mL | 2.2463 mL | 5.6156 mL | |
| 20 mM | 0.1685 mL | 0.8423 mL | 1.6847 mL | 4.2117 mL | |
| 25 mM | 0.1348 mL | 0.6739 mL | 1.3478 mL | 3.3694 mL | |
| 30 mM | 0.1123 mL | 0.5616 mL | 1.1231 mL | 2.8078 mL | |
| 40 mM | 0.0842 mL | 0.4212 mL | 0.8423 mL | 2.1059 mL | |
| 50 mM | 0.0674 mL | 0.3369 mL | 0.6739 mL | 1.6847 mL | |
| 60 mM | 0.0562 mL | 0.2808 mL | 0.5616 mL | 1.4039 mL | |
| 80 mM | 0.0421 mL | 0.2106 mL | 0.4212 mL | 1.0529 mL | |
| 100 mM | 0.0337 mL | 0.1685 mL | 0.3369 mL | 0.8423 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.
Fenspiride hydrochloride Related Classifications
HY-A0027 Related Classifications
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