10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 11 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Loperamide HCl (ADL 2-1294) is a selectiveμ-opioid receptoragonist opioid withKiof 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bow
In vitro
Loperamide exhibits potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently stimulates [35S]guanosine-5\'-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM.
In vivo
Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
| Isomeric SMILES | CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl |
|---|---|
| WGK Germany | 3 |
| RTECS | TM4960000 |
| Molecular Weight | 513.5 |
| Reaxy-Rn | 4087090 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4087090&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →| Solubility | Solubility (25°C) In vitro DMSO: 82 mg/mL (199.08 mM); Water: 82 mg/mL (199.08 mM); Ethanol: 82 mg/mL (199.08 mM); |
|---|---|
| Melt Point(°C) | 223°C |
| 1. Xiao-yan Chang, Yuan-yuan Liu, Meng-meng Hu, You-qian Liu, Cui-hua Jiang, Qi Wang, Qiao-mei Jin, Dong-jian Zhang, Zhi-qi Yin, Jian Zhang. (2022) Comparative effects of different enzymatic hydrolysates of konjac glucomannan on gut flora and constipation in rats. Food & Function, 13 (16): (8717-8729). [PMID:35916206] [10.1039/D2FO01144A] |
| 2. Tian Li, Mengmeng Hu, Cuihua Jiang, Dongjian Zhang, Meng Gao, Jianwei Xia, Mengqi Miao, Gaofeng Shi, Hui Li, Jian Zhang, Zhiqi Yin. (2020) Laxative effect and mechanism of Tiantian Capsule on loperamide-induced constipation in rats. JOURNAL OF ETHNOPHARMACOLOGY, [PMID:32980482] [10.1016/j.jep.2020.113411] |
| 3. Jiayi Ma, Yan Su, Jingru Xie, Lin Tao, Yan Zhao, Xiaoxia Wang, Zhenying Kuang, Xianjie Sheng, An Kang, Jiye Aa, Guangji Wang. (2024) Chemometric-based analysis and bioassay guided identification of potent compounds with intestinal motility promoting effects from Dalitong Granules. JOURNAL OF ETHNOPHARMACOLOGY, [PMID:39236779] [10.1016/j.jep.2024.118777] |
| 4. Jingyu Gao, Fan Wu, Mingzhu Yan, Xuejiang Wang, Yan Chi, Yu Zhang, Yu Peng, Mo Li, Yuanying Ni, Xin Wen. (2024) Effects of brown seaweed oligosaccharides on obesity and constipation managements. JOURNAL OF FOOD SCIENCE, 90 (1): (e17647). [PMID:39736091] [10.1111/1750-3841.17647] |
| 5. Liao Yiqi, Wang Yanfang, Huang Weirui, Wang Junxiang, Guo Mu, Zhang Jiahui, Zheng Hanlu, Yan Yingxue, Lin Zhaolong, Qiu Nengfu, Yu Xiangbin, Yu Yue. (2024) L. acidophilus/L. johnsonii ratio affects slow transit constipation in rats. Scientific Reports, 14 (1): (1-13). [PMID:39256411] [10.1038/s41598-024-71945-8] |
| 6. Dandan Li, Haodong Yan, Junjuan Yu, Yujun Huang, Lina Pan, Wenli Kang, Rongxue Tang, Jiaqi Wang, Hengxian Qu, Yunchao Wa, Xia Chen, Ruixia Gu, Chenchen Zhang. (2024) Probiotic effects of human milk-derived Lactiplantibacillus plantarum M660 on mice with antibiotic-associated diarrhoea and constipation. INTERNATIONAL JOURNAL OF DAIRY TECHNOLOGY, [PMID:] [10.1111/1471-0307.13159] |
| 7. Huaxian Chen, Xingyang Wan, Qiulan He, Guozhong Xiao, Yihui Zheng, Minyi Luo, Chaoxin Yang, Donglin Ren, Li Lu, Hui Peng, Hongcheng Lin. (2024) Single-cell RNA sequencing reveals cellular dynamics and therapeutic effects of astragaloside IV in slow transit constipation. Biomolecules and Biomedicine, [PMID:38289380] [10.17305/bb.2024.10187] |
| 8. Zhiqin Liu, Yufeng Xu, Wei Liu, Lin Wang, Zhen Dong, Jianguo Zeng. (2025) Macleaya cordata protopine total alkaloids as potential treatment for diarrhoea: Mechanistic insights and target identification. RESEARCH IN VETERINARY SCIENCE, [PMID:40184723] [10.1016/j.rvsc.2025.105633] |
| 9. Junnan Wu, Qilei Xin, Shuo Wang, Xu Zhang, Chunping Jiang. (2025) Aqueous extracts of Elsholtzia ciliata and Hovenia dulcis ameliorate loperamide-induced constipation in mice by promoting intestinal peristalsis and barrier function and the abundance of intestinal beneficial bacteria. Frontiers in Microbiology, [PMID:40432966] [10.3389/fmicb.2025.1531232] |
| 10. Yun Wang, Simin Zheng, Hao Zheng, Yangru Huang, Bowen Liang, Yingfei Gong, Jinhai Shen, Wenrui Liu, Xiaona Xu, Yuliang Ma, Zhen Liu. (2026) L-arabinose attenuates loperamide-induced constipation through regulation of gut microbiota in mice. Food & Function, [PMID:41699997] [10.1039/D4FO03554B] |
| 11. Yangyang Zhang, Xia Cao, Zong Hou, Zhiqiang Liu, Shu Liu. (2026) Dual benefits of Xiao Chai Hu Tang and its active compounds in CPT-11 therapy: intestinal protection via barrier restoration and anti-inflammation combined with enhanced tumor apoptosis. JOURNAL OF ETHNOPHARMACOLOGY, [PMID:] [10.1016/j.jep.2026.121621] |
