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/ Fenspiride HCl

芬司匹利盐酸盐 /Fenspiride HCl {[allProObj[0].p_purity_real_show]}

货号：A188332 同义名： 盐酸芬司必利;芬司必利盐酸盐 / Fenspiride (hydrochloride);Decaspiride

Fenspiride HCl is an antagonist of α-adrenergic receptors and H1 histamine receptors and also inhibits phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively.

Fenspiride HCl 化学结构 CAS号：5053-08-7
Fenspiride HCl 化学结构
CAS号：5053-08-7
Fenspiride HCl 3D分子结构
CAS号：5053-08-7
Fenspiride HCl 化学结构 CAS号：5053-08-7
Fenspiride HCl 3D分子结构 CAS号：5053-08-7
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Fenspiride HCl 纯度/质量文件 产品仅供科研

货号：A188332 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ 98%
Maprotiline hydrochloride ✔ 98%
Cisatracurium besylate ✔ 98%
Yohimbine HCI ✔ 99+%
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

 		+

β1-adrenoceptor, pIC50: 5.1

 		97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

 		97%
Piribedil ++

adrenoceptor α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

 		98%
Prazosin HCl ✔ 95%
Silodosin ✔ 98%
Phenoxybenzamine HCl ✔ 98%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

 		98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		97%
Alfuzosin HCl ✔ 98%
Terazosin HCl ✔ 99%
Atipamezole ✔ 95%
Phentolamine methanesulfonate salt ✔ 99%
Doxazosin mesylate ✔ 98%
Tolazoline HCl ✔ 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine dihydrochloride ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		98%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 98%
Levodropropizine ✔ 97%
Cyproheptadine hydrochloride ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin hydrochloride ✔ 99+%
Buclizine 2HCl ✔ 97%
Latrepirdine 2HCl ✔ GluR 98%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Fenspiride HCl 生物活性

靶点

  • PDE4

    PDE4, pIC50:4.16

  • PDE3

    PDE3, pIC50:3.44
描述 Fenspiride hydrochloride is used in treating chronic inflammatory diseases, most commonly as a liquid oral solution[3]. Fenspiride is an antagonist of H1-histamine receptors that is used to treat acute and chronic respiratory tract infections and otitis media in children and adolescents. Long-term administration of fenspiride has no negative impact on BMD(bone mineral density) and bone metabolism in young growing rats[4]. Moreover, Fenspiride administration to rats during the acute stage of COPD(Chronic obstructive pulmonary disease) (15 days of NO2 exposure) prevented the bronchial constriction induced by NO2[5].

Fenspiride HCl 参考文献

[1]Cortijo J, Naline E, 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.

[2]Cunha FQ, Boukili MA, et al. Blockade by fenspiride of endotoxin-induced neutrophil migration in the rat. Eur J Pharmacol. 1993 Jul 6;238(1):47-52.

[3]Cioroiu BI, Caba IC, Prisăcaru I, Cioroiu ME, Lazar MI, Niculaua M. New approach for determination of the degradation products of fenspiride hydrochloride found in oral liquid formulations. Biomed Chromatogr. 2018 May;32(5):e4176. doi: 10.1002/bmc.4176. Epub 2018 Jan 22. PMID: 29265479.

[4]Matuszewska A, Nowak B, Jędrzejuk D, Landwójtowicz M, Bolanowski M, Dziewiszek W, Merwid-Ląd A, Szeląg E, Zduniak K, Kwiatkowska J, Szeląg A. 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. doi: 10.17219/acem/93729. PMID: 30843675.

[5]Kuzubova NA, Lebedeva ES, Fedin AN, Dvorakovskaya IV, Preobrazhenskaya TN, Titova ON. Effect of fenspiride on bronchial smooth muscle of rats with chronic obstructive pulmonary disease. J Smooth Muscle Res. 2013;49:46-54. doi: 10.1540/jsmr.49.46. PMID: 24133694; PMCID: PMC5137255.

Fenspiride HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.37mL

0.67mL

0.34mL

16.85mL

3.37mL

1.68mL

33.69mL

6.74mL

3.37mL

Fenspiride HCl 技术信息

CAS号5053-08-7
分子式C15H21ClN2O2
分子量 296.792
别名 盐酸芬司必利;芬司必利盐酸盐;盐酸芬司匹利 ;Fenspiride (hydrochloride);Decaspiride;Fenspiride hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 35 mg/mL(117.93 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(168.47 mM)，配合低频超声助溶
动物实验配方

PO 0.5% CMC-Na 120 mg/mL clear

Tags: Fenspiride | 5053-08-7 | PDE3/PDE4/PDE5/HRH1 Inhibitor | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Metabolic Enzyme/Protease | Histamine Receptor | Phosphodiesterase (PDE) | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Fenspiride HCl 纯度/质量文件 | Fenspiride HCl 亚型比较 | Fenspiride HCl 生物活性 | Fenspiride HCl 参考文献 | Fenspiride HCl 实验方案 | Fenspiride HCl 技术信息

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