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/ Racecadotril/消旋卡多曲

Racecadotril/消旋卡多曲 {[allProObj[0].p_purity_real_show]}

货号：A148453 同义名： Acetorphan

Racecadotril是一种内啡肽酶抑制剂，IC50 为 4.5 μM，用于治疗腹泻，能够通过抑制内啡肽酶活性发挥作用。

Racecadotril/消旋卡多曲 化学结构 CAS号：81110-73-8
Racecadotril/消旋卡多曲 化学结构
CAS号：81110-73-8
Racecadotril/消旋卡多曲 3D分子结构
CAS号：81110-73-8
Racecadotril/消旋卡多曲 化学结构 CAS号：81110-73-8
Racecadotril/消旋卡多曲 3D分子结构 CAS号：81110-73-8
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Racecadotril/消旋卡多曲 纯度/质量文件 产品仅供科研

货号：A148453 标准纯度： {[allProObj[0].p_purity_real_show]}
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Racecadotril/消旋卡多曲 生物活性

靶点

  • Opioid receptor
描述 Racecadotril, via its active metabolite thiorphan, is an inhibitor of the enzyme neutral endopeptidase (NEP, EC 3.4.24.11), thereby increasing exposure to NEP substrates including enkephalins and atrial natriuretic peptide (ANP). Upon oral administration racecadotril is rapidly and effectively converted into the active metabolite thiorphan, which does not cross the blood-brain-barrier[3]. Orally administered Racecadotril (100 mg/kg) shows efficacy in a rat model of castor oil-induced diarrhea[4]. Racecadotril is used in the treatment of acute diarrhoea. It prevents the degradation of endogenous opioids (enkephalins), thereby reducing hypersecretion of water and electrolytes into the intestinal lumen. In well controlled trials, racecadotril had efficacy similar to that of loperamide and was generally as effective as loperamide-oxide. In well controlled trials, racecadotril had efficacy similar to that of loperamide and was generally as effective as loperamide-oxide[5]. Racecadotril is more efficacious than other treatments except for loperamide and has a tolerability similar to placebo and better than loperamide[6].

Racecadotril/消旋卡多曲 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02125604 Relapsing-Remitting Multiple S... 展开 >>clerosis 收起 << Phase 4 Completed - Germany ... 展开 >> Research Site Augsburg, Germany Research Site Bamburg, Germany Research Site Bayreuth, Germany Research Site Berlin, Germany Research Site Bochum, Germany Research Site Bonn, Germany Research Site Erbach, Germany Research Site Erlangen, Germany Research Site Freiburg, Germany Research Site Hamburg, Germany Research Site Leipzig, Germany Research Site Marburg, Germany Research Site Minden, Germany Research Site Mittweida, Germany Research Site Munchen, Germany Research Site Munster, Germany Research Site Osnabruck, Germany Research Site Potsdam, Germany Research Site Siegen, Germany 收起 <<
NCT03005821 Diarrhea Not Applicable Recruiting September 30, 2019 China, Guangdong ... 展开 >> Dongguan Kanghua Hospital Recruiting Dongguan, Guangdong, China, 523080 Contact: Lingjia Yin, Physician    8613112843921    632608836@qq.com 收起 <<
NCT00940290 - Completed - -

Racecadotril/消旋卡多曲 参考文献

[1]Marion Eberlin, Tobias Muck, et al. A Comprehensive Review of the Pharmacodynamics, Pharmacokinetics, and Clinical Effects of the Neutral Endopeptidase Inhibitor Racecadotril. Front Pharmacol. 2012; 3: 93.

[2]Wu HT, Chang CK, et al. Increase of plasma insulin by racecadotril, an inhibitor of enkephalinase, in Wistar rats. Horm Metab Res. 2010 Apr;42(4):261-7.

[3]Eberlin M, Mück T, Michel MC. A comprehensive review of the pharmacodynamics, pharmacokinetics, and clinical effects of the neutral endopeptidase inhibitor racecadotril. Front Pharmacol. 2012 May 30;3:93

[4]Griggs DW, Prinsen MJ, Oliva J, Campbell MA, Arnett SD, Tajfirouz D, Ruminski PG, Yu Y, Bond BR, Ji Y, Neckermann G, Choy RK, de Hostos E, Meyers MJ. Pharmacologic Comparison of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea. J Pharmacol Exp Ther. 2016 May;357(2):423-31

[5]Matheson AJ, Noble S. Racecadotril. Drugs. 2000 Apr;59(4):829-35; discussion 836-7

[6]Eberlin M, Chen M, Mueck T, Däbritz J. Racecadotril in the treatment of acute diarrhea in children: a systematic, comprehensive review and meta-analysis of randomized controlled trials. BMC Pediatr. 2018 Apr 3;18(1):124

Racecadotril/消旋卡多曲 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.97mL

2.59mL

1.30mL

25.94mL

5.19mL

2.59mL

Racecadotril/消旋卡多曲 技术信息

CAS号81110-73-8
分子式C21H23NO4S
分子量 385.48
SMILES Code O=C(OCC1=CC=CC=C1)CNC(C(CC2=CC=CC=C2)CSC(C)=O)=O
MDL No. MFCD00865520
别名 Acetorphan
运输蓝冰
InChI Key ODUOJXZPIYUATO-UHFFFAOYSA-N
Pubchem ID 107751
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, sealed in dry, room temperature
溶解方案

DMSO: 105 mg/mL(272.39 mM)，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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Racecadotril | 81110-73-8 | Acetorphan | Neprilysin | Metabolic Enzyme/Protease | Neprilysin | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Racecadotril/消旋卡多曲 纯度/质量文件 | Racecadotril/消旋卡多曲 生物活性 | Racecadotril/消旋卡多曲 临床数据 | Racecadotril/消旋卡多曲 参考文献 | Racecadotril/消旋卡多曲 实验方案 | Racecadotril/消旋卡多曲 技术信息

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