Home Metabolism PDE inhibitor Fenspiride HCl

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Fenspiride HCl PDE inhibitor

Cat.No.S4090

Fenspiride(Decaspiride) is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.
Fenspiride HCl PDE inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 296.79

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Quality Control

Batch: S409001 Water]59 mg/mL]false]DMSO]9 mg/mL]false]Ethanol]Insoluble]false Purity: 99.91%
99.91

Chemical Information, Storage & Stability

Molecular Weight 296.79 Formula

C15H20N2O2.HCl

 Storage (From the date of receipt)
CAS No. 5053-08-7 Download SDF Storage of Stock Solutions

Synonyms Decaspiride Smiles C1CN(CCC12CNC(=O)O2)CCC3=CC=CC=C3.Cl

Solubility

In vitro
Batch:

Water : 59 mg/mL

DMSO : 9 mg/mL (30.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Features
Produces less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities.
Targets/IC50/Ki
PDE4 [1]
4.16(pIC50)
PDE3 [1]
3.44(pIC50)
In vitro

Fenspiride induces potentiation of the effects of isoprenaline and sodium nitroprusside with logEC50 of 4.1 and 3.5, respectively, in human isolated bronchi. [1]
In vivo

Fenspiride, an antiinflammatory drug with low anti-cyclooxygenase activity, administered orally at 60-200 mg/kg inhibits neutrophil migration into peritoneal and air pouches cavities as well as exudation into peritoneal cavities induced by endotoxin but not induced by carrageenin in the rat. Fenspiride (200 mg/kg) inhibits the release of tumour necrosis factor by stimulated macrophages in a dose-dependent manner in the rat. [2] Fenspiride (Topically applied) is found to inhibit the development of sclerotic lesions in myringotomized rats, whereas intraperitoneal injections are ineffective. [3] Fenspiride (60 mg/kg) significantly reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum (4.2 ng/mL vs. 2.3 ng/mL) and in the bronchoalveolar lavage fluid (55.7 ng/mL vs. 19.7 ng/mL) of guinea-pigs with endotoxemia. Fenspiride (60 mg/kg) also significantly reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages, defined as their enhanced release of arachidonic acid metabolites as compared to cells from untreated controls upon stimulation with N-formyl-methionyl-phenylalanine. Fenspiride (60 mg/kg) reduces the increased serum concentrations of extracellular type II phospholipase A2, the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide in guinea-pigs with endotoxemia. [4]
References

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