Loperamide hydrochloride
Based on 13 publication(s) in Google Scholar
Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 34552-83-5
- Formula: C29H34Cl2N2O2
- Molecular Weight:513.50
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Loperamide hydrochloride
More- Nature. 2025 Dec;648(8094):755-763. [Abstract]
- Phytomedicine. 2025 Nov 25:148:157417. [Abstract]
- J Transl Med. 2021 Jul 23;19(1):317. [Abstract]
- Int J Biol Macromol. 2026 Apr:357:151532. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- eFood. 2025 Jul 14.
- Food Qual Saf. 2024 Sep 10.
- Oncol Rep. 2025 Oct;54(4):133. [Abstract]
- Viruses. 2021 Jun 28;13(7):1255. [Abstract]
- Neurogastroenterol Motil. 2026 Apr;38(4):e70298. [Abstract]
- Dig Dis Sci. 2025 Nov 15. [Abstract]
- J Appl Microbiol. 2023 Aug 1;134(8):lxad153. [Abstract]
- Curr Med Sci. 2025 Aug 29. [Abstract]
All Opioid Receptor Isoforms
More
Biological Activity
Loperamide (17.5 µM, 1-48 h) induces hallmarks of ER stress and autophagy in GBM cells and MEFs[5].
Loperamide (17.5 µM, 48 h) decrease in LC3B and GABARAP lipidation levels in ATF4 KO cells compared to WT cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GBM cell and mouse embryonic fibroblasts (MEFs)
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Concentration:17.5 µM
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Incubation Time:1, 2, 4, 6, 8, 24, 30, 48 h
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Result:Increased the levels of the major chaperone HSPA5 in both cell lines.
Chemical Information
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CAS No. 34552-83-5
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Appearance Solid
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Molecular Weight 513.50
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Formula C29H34Cl2N2O2
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Color White to off-white
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SMILES
O=C(N(C)C)C(C1=CC=CC=C1)(C2=CC=CC=C2)CCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3.Cl
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Synonyms
R-18553 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nature
2025 Dec;648(8094):755-763. PMID: 41193810 -
Phytomedicine
Xiaoer Qixing Cha alleviates functional constipation via regulating gut microbiota and short-chain fatty acids in mice. [Abstract]2025 Nov 25:148:157417. PMID: 41161186 -
J Transl Med
Constipation induced gut microbiota dysbiosis exacerbates experimental autoimmune encephalomyelitis in C57BL/6 mice. [Abstract]2021 Jul 23;19(1):317. PMID: 34301274 -
Int J Biol Macromol
L-β-Galactoglucan alleviates loperamide-induced constipation in mice and regulates gut microbiota and metabolism. [Abstract]2026 Apr:357:151532. PMID: 41887441 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
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Oncol Rep
2025 Oct;54(4):133. PMID: 40776759 -
Viruses
Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]2021 Jun 28;13(7):1255. PMID: 34203149 -
Neurogastroenterol Motil
Acacetin Alleviates Loperamide-Induced Functional Constipation by Inhibiting P53-Mediated Apoptosis in Colonic Epithelial Cells. [Abstract]2026 Apr;38(4):e70298. PMID: 41913080 -
Dig Dis Sci
Kaempferol Ameliorates Functional Constipation in Mice by Regulating Autophagy of Interstitial Cells of Cajal via the p53/AMPK/mTOR Axis. [Abstract]2025 Nov 15. PMID: 41240265 -
J Appl Microbiol
Houpo Paiqi Mixture Promotes Intestinal Motility in Constipated Rats by Modulating Gut Microbiota and Activating 5-HT-cAMP-PKA Signal Pathway. [Abstract]2023 Aug 1;134(8):lxad153. PMID: 37481692 -
Curr Med Sci
Konjac Oligosaccharide Alleviates Constipation in Mice via 5-HT4R/cAMP/PKA/p-CREB Pathway Activation. [Abstract]2025 Aug 29. PMID: 40879997
Solvent & Solubility
DMSO : 43.75 mg/mL (85.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (1.95 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Hanauer, S.B., The role of loperamide in gastrointestinal disorders. Rev Gastroenterol Disord, 2008. 8(1): p. 15-20. [Content Brief]
[2]. Litovitz, T., et al., Surveillance of loperamide ingestions: an analysis of 216 poison center reports. J Toxicol Clin Toxicol, 1997. 35(1): p. 11-9. [Content Brief]
[3]. http://www.drugs.com/mmx/loperamide-hydrochloride.html
[4]. Hatfield MJ, et al. Carboxylesterase inhibitors. Expert Opin Ther Pat. 2011 Aug;21(8):1159-71. [Content Brief]
[5]. Svenja Zielke, et al. ATF4 links ER stress with reticulophagy in glioblastoma cells. Autophagy. 2021, 17, 9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9474 mL | 9.7371 mL | 19.4743 mL | 48.6856 mL |
| DMSO | 5 mM | 0.3895 mL | 1.9474 mL | 3.8949 mL | 9.7371 mL |
| 10 mM | 0.1947 mL | 0.9737 mL | 1.9474 mL | 4.8686 mL | |
| 15 mM | 0.1298 mL | 0.6491 mL | 1.2983 mL | 3.2457 mL | |
| 20 mM | 0.0974 mL | 0.4869 mL | 0.9737 mL | 2.4343 mL | |
| 25 mM | 0.0779 mL | 0.3895 mL | 0.7790 mL | 1.9474 mL | |
| 30 mM | 0.0649 mL | 0.3246 mL | 0.6491 mL | 1.6229 mL | |
| 40 mM | 0.0487 mL | 0.2434 mL | 0.4869 mL | 1.2171 mL | |
| 50 mM | 0.0389 mL | 0.1947 mL | 0.3895 mL | 0.9737 mL | |
| 60 mM | 0.0325 mL | 0.1623 mL | 0.3246 mL | 0.8114 mL | |
| 80 mM | 0.0243 mL | 0.1217 mL | 0.2434 mL | 0.6086 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Loperamide hydrochloride Related Classifications
HY-B0418A Related Classifications
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