Loperamide HCl

For research use only.

Catalog No.S2480 Synonyms: ADL 2-1294

5 publications

Loperamide HCl Chemical Structure

CAS No. 34552-83-5

Loperamide HCl (ADL 2-1294) is a selective μ-opioid receptor agonist opioid with Ki of 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 bowel disease.

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10mM (1mL in DMSO) EUR 127 In stock
EUR 95 In stock
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Selleck's Loperamide HCl has been cited by 5 publications

2 Customer Reviews

  • Low-micromolar amounts of loperamide inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 8 μM LPM (C). Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.

    Antimicrob Agents Chemother, 2014, 58(8):4875-4884.. Loperamide HCl purchased from Selleck.

    Comparison of transit from the stomach over 12 h for animals treated with different concentrations of loperamide, prucalopride, and for DMSO-treated/control animals (dotted line) at 4 h (black), 9 h (light grey), and 12 h (dark grey) (n = 7–13 animals per group). (A) The percentage of rats in which all beads had exited the stomach, and (B) the percentage of beads that had exited the stomach (mean per treatment). Asterisks indicate the significance of each treatment relative to controls (*p < 0.05). Data show mean±SEM

    Neurogastroenterol Motil, 2016, 28(8):1241-51. Loperamide HCl purchased from Selleck.

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Biological Activity

Description Loperamide HCl (ADL 2-1294) is a selective μ-opioid receptor agonist opioid with Ki of 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 bowel disease.
μ-opioid receptor [1]
δ-opioid receptor [1]
3.3 nM(Ki) 48 nM(Ki)
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). [1] 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). [2] 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. [3]

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. [4]


Solubility (25°C)

In vitro DMSO 22 mg/mL (42.84 mM)
Water Insoluble
Ethanol '4 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+H2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 513.5


CAS No. 34552-83-5
Storage powder
in solvent
Synonyms ADL 2-1294
Smiles CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04225078 Suspended Drug: Loperamide|Other: Placebo|Drug: Moxifloxacin Healthy Participants Janssen Research & Development LLC January 17 2020 Phase 1
NCT03489265 Withdrawn Drug: Eluxadoline 100 mg|Other: Placebo Fecal Incontinence|Accidental Bowel Leakage|Anal Incontinence|Diarrhea|Urge Incontinence University of North Carolina Chapel Hill|Allergan April 2019 Phase 2
NCT02677844 Completed Drug: Abemaciclib|Drug: Placebo|Drug: Loperamide Healthy Eli Lilly and Company February 2016 Phase 1
NCT02628626 Recruiting Drug: Colesevelam|Drug: Clonidine|Other: Placebo Fecal Incontinence|Bile Acid Malabsorption Mayo Clinic November 2015 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID