| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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| 50g |
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| Other Sizes |
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Purity: ≥98%
Fenspiride (NAT-333; JP-428; NDR-5998A; Decaspiride; Espiran; trade names Eurespal, Pneumorel), an oxazolidinone spiro compound acting as a α adrenergic and H1 histamine receptor antagonist, is a bronchodilator with potent anti-inflammatory properties. Iit inhibits phosphodiesterase 4/3 (PDE4/3) with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi. Fenspiride is an oxazolidinone spiro compound used as a drug in the treatment of certain respiratory diseases.
| ln Vitro |
The histamine-induced contraction of isolated guinea pig trachea is inhibited by fenspiride (at approximately 100 μM)[2]. Less than 25% of phosphodiesterase 1 and phosphodiesterase 2 activities are inhibited by fenspiride (≤1000 μM)[2].
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| ln Vivo |
The lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum and bronchoalveolar lavage fluid (BALF) of the endotoxemia model is lessened by fenspiride (60 mg/kg; po for 3 days)[3]. Alveolar macrophages' primed activation caused by lipopolysaccharide is lessened by fenspiride (60 mg/kg; po for 3 days)[3]. The increased serum concentrations of extracellular type II phospholipase A 2, the severity of neutrophilic alveolar invasion, and the mortality resulting from lipopolysaccharide are all decreased by fenspiride (60 mg/kg; po for 3 days)[3].
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| Animal Protocol |
Animal/Disease Models: Lipopolysaccharide-treated Male Dunkin-Hartley guinea-pigs weighing 400-600 g[3]
Doses: 60 mg/kg Route of Administration: Orally for 3 days; pretreated Experimental Results: decreased 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). decreased 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). decreased 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. |
| References |
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| Molecular Formula |
C15H20N2O2.HCL
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|---|---|
| Molecular Weight |
296.79
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| Exact Mass |
296.129
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| CAS # |
5053-08-7
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| Related CAS # |
Fenspiride;5053-06-5;Fenspiride-d5;1246911-67-0
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| PubChem CID |
68626
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| Appearance |
White to off-white solid powder
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| Density |
1.19g/cm3
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| Boiling Point |
474.3ºC at 760mmHg
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| Melting Point |
235-238ºC (dec.)
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| Flash Point |
240.6ºC
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| LogP |
2.872
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
318
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FIKFLLIUPUVONI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H20N2O2.ClH/c18-14-16-12-15(19-14)7-10-17(11-8-15)9-6-13-4-2-1-3-5-13;/h1-5H,6-12H2,(H,16,18);1H
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| Chemical Name |
8-(2-Phenylethyl)-1-oxa-3,8-diazaspiro(4.5)decan-2-one hydrochloride
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| Synonyms |
NAT333; NAT 333; JP 428; JP428; NDR-5998A; NDR 5998A; NAT-333; JP-428; NDR5998A; Decaspiride; Espiran; Fenspiride HCl; Fenspiride hydrochloride; Fluiden. trade names Eurespal, Pneumorel
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (9.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (9.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (9.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (404.33 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3694 mL | 16.8469 mL | 33.6939 mL | |
| 5 mM | 0.6739 mL | 3.3694 mL | 6.7388 mL | |
| 10 mM | 0.3369 mL | 1.6847 mL | 3.3694 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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