Loperamide HCl

Catalog No.S2480 Batch:S248002

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Technical Data

Formula

C29H33ClN2O2.HCl

Molecular Weight 513.5 CAS No. 34552-83-5
Solubility (25°C)* In vitro DMSO 24 mg/mL (46.73 mM)
Ethanol 4 mg/mL (7.78 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
7.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) 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.
Targets
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]

Protocol (from reference)

Customer Product Validation

, , Antimicrob Agents Chemother, 2014, 58(8):4875-4884.

Data from [Data independently produced by , , Neurogastroenterol Motil, 2016, 28(8):1241-51]

Selleck's Loperamide HCl has been cited by 7 publications

Slowed gastrointestinal transit is associated with an altered caecal microbiota in an aged rat model [ Front Cell Infect Microbiol, 2023, 13:1139152] PubMed: 36998634
Assessment in vitro of interactions between anti-cancer drugs and noncancer drugs commonly used by cancer patients [ Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344] PubMed: 36066384
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734] PubMed: 32511305
miR-21 enhances the protective effect of loperamide on rat cardiomyocytes against hypoxia/reoxygenation, reactive oxygen species production and apoptosis via regulating Akap8 and Bard1 expression. [ Exp Ther Med, 2019, 17(2):1312-1320] PubMed: 30680008
Gastric Emptying and Gastrointestinal Transit Compared among Native and Hydrolyzed Whey and Casein Milk Proteins in an Aged Rat Model. [ Nutrients, 2017, 9(12)] PubMed: 29236034
Tracking gastrointestinal transit of solids in aged rats as pharmacological models of chronic dysmotility. [Dalziel JE, et al. Neurogastroenterol Motil, 2016, 28(8):1241-51] PubMed: 27028044
Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture [de Wilde AH, et al. Antimicrob Agents Chemother, 2014, 58(8):4875-84] PubMed: 24841269

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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