Loperamide HCl (R-18553)

Alias: R 18553; ADL-2-1294; R-18553; ADL2-1294; R18553; ADL 2-1294; Loperamide Hydrochloride; Loperamide HCl; Imodium; Dissenten; Fortasec; Loperamide Monohydrochloride
Cat No.:V1273 Purity: ≥98%
Loperamide HCl (R18553; ADL-2-1294; R-18553; ADL 2-1294; Imodium; Dissenten; Fortasec), the hydrochloride salt of loperamide, is a potent and selective μ-opioid receptor agonist used to reduce the frequency of diarrhea, also for IBD-inflammatory bowel disease and short bowel syndrome.
Loperamide HCl (R-18553) Chemical Structure CAS No.: 34552-83-5
Product category: Opioid Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Loperamide HCl (R-18553):

  • Loperamide D6 HCl
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Loperamide HCl (R18553; ADL-2-1294; R-18553; ADL 2-1294; Imodium; Dissenten; Fortasec), the hydrochloride salt of loperamide, is a potent and selective μ-opioid receptor agonist used to reduce the frequency of diarrhea, also for IBD-inflammatory bowel disease and short bowel syndrome. It exhibits selectivity over the δ and κ subtypes of the opioid receptor by 15 and 350 times, respectively, and activates the μ-opioid receptor with a Ki of 3.3 nM. Due to its selective nature towards μ-opioid receptors and restricted brain penetration, Loperamide is unable to exhibit the central systemic effects commonly linked to opiates.

Biological Activity I Assay Protocols (From Reference)
Targets
μ-opioid receptor ( Ki = 3.3 nM ); δ-opioid receptor ( Ki = 48 nM )
ln Vitro

In vitro activity: Loperamide shows potent selectivity and affinity for the cloned micro opioid receptor (Ki = 3 nM) as well as delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor and potently stimulates [35S]guanosine-5'-O-(3-thio)triphosphate binding (EC50 = 56 nM). With an intrapaw injection, limpetamide significantly reduces late-phase formalin-induced flinching (A50 = 6 mg). (Source: ) With an IC50 of 0.44 mM, loperamide only weakly inhibits CES1A1, but it is a strong inhibitor of CES2, with a K(i) of 1.5 muM.[2] Loperamide has a concentration-dependent IC50 of 0.9 mM and reversibly inhibits increases in [Ca2+]i induced by high [K+]. At the highest concentration tested, loperamide (0.1–50 mM) could completely block IBa in the absence of any other pharmacological agent. It also causes a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM. Additionally, loperamide, with an IC50 of 73 mM, attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV.[3]

ln Vivo
Loperamide, an opioid agonist that cannot pass through the blood-brain barrier, when injected subcutaneously (s.c.) under the fur of the neck (4 mg/kg) or locally over the tibial tumoral mass (7.5-75 mg), inhibits both mechanical and thermal hyperalgesia in mice.[4]
Cell Assay
Cell Line: GBM cell and mouse embryonic fibroblasts (MEFs)
Concentration: 17.5 µM
Incubation Time: 1, 2, 4, 6, 8, 24, 30, 48 h
Result: Increased the levels of the major chaperone HSPA5 in both cell lines.
Animal Protocol
4 mg/kg
Mice
References

[1]. J Pharmacol Exp Ther . 1999 Apr;289(1):494-502.

[2]. J Pharmacol Exp Ther . 2005 Jun;313(3):1011-6.

[3]. Mol Pharmacol . 1994 Apr;45(4):747-57.

[4]. Pharmacol Biochem Behav . 2005 May;81(1):114-21.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H34CL2N2O2
Molecular Weight
513.5
Exact Mass
512.2
Elemental Analysis
C, 67.83; H, 6.67; Cl, 13.81; N, 5.46; O, 6.23
CAS #
34552-83-5
Appearance
White to light yellow solid powder
SMILES
CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl
InChi Key
PGYPOBZJRVSMDS-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H33ClN2O2.ClH/c1-31(2)27(33)29(24-9-5-3-6-10-24,25-11-7-4-8-12-25)19-22-32-20-17-28(34,18-21-32)23-13-15-26(30)16-14-23;/h3-16,34H,17-22H2,1-2H3;1H
Chemical Name
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide;hydrochloride
Synonyms
R 18553; ADL-2-1294; R-18553; ADL2-1294; R18553; ADL 2-1294; Loperamide Hydrochloride; Loperamide HCl; Imodium; Dissenten; Fortasec; Loperamide Monohydrochloride
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~22 mg/mL (~42.8 mM)
Water: <1 mg/mL
Ethanol: ~4 mg/mL (~7.8 mM)
Solubility (In Vivo)
5%DMSO + Corn oil: 7.5mg/ml (14.61mM) (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9474 mL 9.7371 mL 19.4742 mL
5 mM 0.3895 mL 1.9474 mL 3.8948 mL
10 mM 0.1947 mL 0.9737 mL 1.9474 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04823065 Recruiting Drug: Loperamide Pill
Drug: hyoscine-n-butylbromide
Endometrial Cancer
Ovarian Cancer
Centre de recherche du Centre
hospitalier universitaire de
Sherbrooke
September 1, 2018 Phase 1
Phase 2
NCT05252988 Recruiting Drug: Neratinib
Drug: Loperamide
Drug: Colesevelam
Early-stage Breast Cancer
HER2 Positive Breast Cancer
Hormone Receptor Positive
Spanish Breast Cancer
Research Group
August 31, 2022 Phase 2
NCT05520723 Recruiting Drug: Sacituzumab govitecan
Drug: Loperamide
Triple Negative Breast Cancer
Breast Cancer
MedSIR February 7, 2023 Phase 2
NCT05677282 Recruiting Drug: Loperamide
Drug: Rifaximin 550 MG
Drug: Azithromycin 500 MG
Diarrhoea;Acute
Diarrhea Travelers
Henry M. Jackson Foundation
for the Advancement
of Military Medicine
October 28, 2022 Phase 4
NCT04186936 Completed Drug: Loperamide HCl
Drug: Simethicone
Healthy McNeil AB December 5, 2019 Phase 1
Contact Us