Catalog No.S2480 Synonyms: ADL 2-1294
Molecular Weight(MW): 513.5
Loperamide HCl 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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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.
Purity & Quality Control
Choose Selective Opioid Receptor Inhibitors
|Description||Loperamide HCl 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.|
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. |
|In vitro||DMSO||22 mg/mL (42.84 mM)|
|Ethanol||4 mg/mL (7.78 mM)|
|In vivo||Add solvents to the product individually and in order:
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.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02686645||Not yet recruiting||Clostridium Difficile Infection||Queen Elizabeth II Health Sciences Centre||December 2016||Phase 2|Phase 3|
|NCT02747004||Recruiting||Metastatic Breast Cancer||Eli Lilly and Company||September 2016||Phase 2|
|NCT02888899||Recruiting||Fecal Incontinence||University Hospital, Linkoeping||March 2016||--|
|NCT02677844||Completed||Healthy||Eli Lilly and Company||February 2016||Phase 1|
|NCT02354768||Recruiting||High Output Stoma||University Hospital, Strasbourg, France|Ipsen||October 2015||Phase 3|
|NCT02441946||Active, not recruiting||Breast Cancer|Hormone Receptor Positive Tumor|Early-Stage Breast Carcinoma||Eli Lilly and Company||August 2015||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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