Home Neuronal Signaling Opioid Receptor agonist - Autophagy activator Loperamide HCl For research use only.

Loperamide HCl

Synonyms: ADL 2-1294,R-18553 hydrochloride

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.

Loperamide HCl Chemical Structure

Loperamide HCl Chemical Structure

CAS No. 34552-83-5

Purity & Quality Control

Loperamide HCl Related Products

Signaling Pathway

Opioid Receptor Signaling Pathways

Opioid Receptor Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04225078 Completed
Healthy Participants
Janssen Research & Development LLC
 January 17 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 513.5 Formula

C29H33ClN2O2.HCl
CAS No. 34552-83-5 SDF Download Loperamide HCl SDF
Smiles CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 27 mg/mL

DMSO : 22 mg/mL ( (42.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Loperamide HCl | Loperamide HCl ic50 | Loperamide HCl price | Loperamide HCl cost | Loperamide HCl solubility dmso | Loperamide HCl purchase | Loperamide HCl manufacturer | Loperamide HCl research buy | Loperamide HCl order | Loperamide HCl mouse | Loperamide HCl chemical structure | Loperamide HCl mw | Loperamide HCl molecular weight | Loperamide HCl datasheet | Loperamide HCl supplier | Loperamide HCl in vitro | Loperamide HCl cell line | Loperamide HCl concentration | Loperamide HCl nmr