1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Metabolic Enzyme/Protease
  2. Histamine Receptor Phosphodiesterase (PDE)
  3. Fenspiride

Fenspiride  (Synonyms: 芬司匹利)

目录号: HY-A0027A
产品使用指南

Fenspiride 是一种口服活性的非甾体抗炎剂,是 H1-组胺受体 (H1-histamine receptors) 的拮抗剂。Fenspiride 抑制磷酸二酯酶 3 (PDE3)、磷酸二酯酶 4 (PDE4)和磷酸二酯酶 5 (PDE5) 的活性,-log IC50 值分别为 3.44、4.16 和大约 3.8。Fenspiride 可用于呼吸系统疾病的研究。

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Fenspiride Chemical Structure

Fenspiride Chemical Structure

CAS No. : 5053-06-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3].

IC50 & Target[2]

H1 Receptor

 

PDE3

 

PDE4

 

PDE5

 

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Fenspiride (60 mg/kg; p.o. for 3 days) reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum and in the bronchoalveolar lavage fluid (BALF) of the model of endotoxemia[3].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Lipopolysaccharide-treated Male Dunkin-Hartley guinea-pigs weighing 400-600 g[3]
Dosage: 60 mg/kg
Administration: orally for 3 days; pretreated
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.
分子量

260.33

Formula

C15H20N2O2

CAS 号
性状

固体

颜色

White to off-white

中文名称

芬司匹利;芬司必利

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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