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/ Loperamide HCl

Loperamide HCl {[allProObj[0].p_purity_real_show]}

货号：A171923 同义名： 盐酸洛哌丁胺 / R-18553 hydrochloride; Loperamide(hydrochloride)

Loperamide HCl是一种强效且选择性的μ-阿片受体激动剂。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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Inaccessible (Haz class 6.1), Domestic USD 80+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Loperamide HCl 化学结构 CAS号：34552-83-5
Loperamide HCl 化学结构
CAS号：34552-83-5
Loperamide HCl 3D分子结构
CAS号：34552-83-5
Loperamide HCl 化学结构 CAS号：34552-83-5
Loperamide HCl 3D分子结构 CAS号：34552-83-5
规格 价格 会员价 库存 数量
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Loperamide HCl 纯度/质量文件 产品仅供科研

货号：A171923 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 Opioid receptor ↓ ORL1 ↓ μ-opioid receptor ↓ 其他靶点 纯度
Racecadotril ✔ 98%
JTC-801 ++

Opioid receptor-like1 (ORL1), IC50: 94 nM

 		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。

Loperamide HCl 生物活性

描述 Loperamide (Hydrochloride) is an opioid receptor agonist widely used for the treatment of diarrhea[3]. In contrast with other opioid agonists, loperamide is a peripherally acting μ-receptor agonist exerting its effects mainly on the myenteric plexus of the gastrointestinal longitudinal muscle layer. It decreases peristalsis and fluid secretion resulting in longer gastrointestinal transit time. The bioavailability of the drug is extremely low. Moreover, it is actively excluded from the central nervous system; hence, it lacks the central effects of euphoria and analgesia at the recommended dosages[4]. Rats were orally gavaged with 1.5, 3, or 6 mg/kg body weight (BW) of loperamide hydrochloride for 7 days. The results after 7 days administration of loperamide, revealed dose-dependent increase in aspartate aminotransferase, lactate dehydrogenase, creatine kinase-MB, and serum concentration of cardiac troponin I, total homocysteine, and nitric oxide. Loperamide provoked cardiotoxicity through oxidative stress, lipid peroxidation, and DNA fragmentation in rats[5]. Loperamide decreased cell viability in a dose-dependent fashion and was most effective against canine osteosarcoma cells. When co-incubated with doxorubicin, loperamide induced a synergistic cell kill in canine carcinoma cells[6].

Loperamide HCl 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
NCT03575078 Lymphoma Phase 1 Not yet recruiting August 23, 2023 -
NCT00555620 - Completed - -
NCT02677844 - Completed - -

Loperamide HCl 参考文献

[1]Hanauer SB. The role of loperamide in gastrointestinal disorders. Rev Gastroenterol Disord. 2008 Winter;8(1):15-20.

[2]Litovitz T, Clancy C, et al. Surveillance of loperamide ingestions: an analysis of 216 poison center reports. J Toxicol Clin Toxicol. 1997;35(1):11-9.

[3]Wu PE, Juurlink DN. Clinical Review: Loperamide Toxicity. Ann Emerg Med. 2017 Aug;70(2):245-252

[4]Akel T, Bekheit S. Loperamide cardiotoxicity: "A Brief Review". Ann Noninvasive Electrocardiol. 2018 Mar;23(2):e12505

[5]Olofinsan KA, Ajala-Lawal RA, Ajiboye TO. Loperamide-induced cardiotoxicity in rats: Evidence from cardiac and oxidative stress biomarkers. J Biochem Mol Toxicol. 2019 Apr;33(4):e22278

[6]Regan RC, Gogal RM Jr, Barber JP, Tuckfield RC, Howerth EW, Lawrence JA. Cytotoxic effects of loperamide hydrochloride on canine cancer cells. J Vet Med Sci. 2014 Dec;76(12):1563-8

Loperamide HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.47mL

3.89mL

1.95mL

Loperamide HCl 技术信息

CAS号34552-83-5
分子式C29H34Cl2N2O2
分子量 513.5
SMILES Code O=C(N(C)C)C(C1=CC=CC=C1)(C2=CC=CC=C2)CCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3.[H]Cl
MDL No. MFCD00058581
别名 盐酸洛哌丁胺 ;R-18553 hydrochloride; Loperamide(hydrochloride); R 18553; PJ 185; NSC 696356; Loperamide hydrochloride; R-18553(hydrochloride)
运输蓝冰
InChI Key PGYPOBZJRVSMDS-UHFFFAOYSA-N
Pubchem ID 71420
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, room temperature
溶解方案

DMSO: 50 mg/mL(97.37 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: 1 mg/mL(1.95 mM)，配合低频超声助溶

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
动物实验配方

2% DMSO+30% PEG 300+water 2.5 mg/mL

Tags: Loperamide | 34552-83-5 | R-18553 | R18553 | R 18553 | Opioid Receptor Agonist | GPCR/G Protein | Neuronal Signaling | Autophagy | Opioid Receptor | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Loperamide HCl 纯度/质量文件 | Loperamide HCl 亚型比较 | Loperamide HCl 生物活性 | Loperamide HCl 临床数据 | Loperamide HCl 参考文献 | Loperamide HCl 实验方案 | Loperamide HCl 技术信息

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