2. GPCR/G Protein Neuronal Signaling Autophagy
  3. Opioid Receptor Autophagy
  4. Loperamide hydrochloride

Loperamide hydrochloride  (Synonyms: R-18553 hydrochloride)

Cat. No.: HY-B0418A Purity: 99.90%
COA Handling Instructions

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Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.

For research use only. We do not sell to patients.

Loperamide hydrochloride Chemical Structure

Loperamide hydrochloride Chemical Structure

CAS No. : 34552-83-5

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10 mM * 1 mL in DMSO
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Based on 5 publication(s) in Google Scholar

Other Forms of Loperamide hydrochloride:

Loperamide hydrochloride Related Antibodies

Top Publications Citing Use of Products

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist[1][2][3]. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect[4].

In Vitro

Loperamide (17.5 µM, 1-48 h) induces hallmarks of ER stress and autophagy in GBM cells and MEFs[5].
Loperamide (17.5 µM, 48 h) decrease in LC3B and GABARAP lipidation levels in ATF4 KO cells compared to WT cells[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Loperamide hydrochloride Related Antibodies

Cell Autophagy Assay[5]

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.
Clinical Trial
Molecular Weight

513.50

Formula

C29H34Cl2N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C)C)C(C1=CC=CC=C1)(C2=CC=CC=C2)CCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 43.75 mg/mL (85.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 1 mg/mL (1.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9474 mL 9.7371 mL 19.4743 mL
5 mM 0.3895 mL 1.9474 mL 3.8949 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.90%

COA (255 KB) RP-HPLC (244 KB) LCMS (258 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9474 mL 9.7371 mL 19.4743 mL 48.6856 mL
DMSO 5 mM 0.3895 mL 1.9474 mL 3.8949 mL 9.7371 mL
10 mM 0.1947 mL 0.9737 mL 1.9474 mL 4.8686 mL
15 mM 0.1298 mL 0.6491 mL 1.2983 mL 3.2457 mL
20 mM 0.0974 mL 0.4869 mL 0.9737 mL 2.4343 mL
25 mM 0.0779 mL 0.3895 mL 0.7790 mL 1.9474 mL
30 mM 0.0649 mL 0.3246 mL 0.6491 mL 1.6229 mL
40 mM 0.0487 mL 0.2434 mL 0.4869 mL 1.2171 mL
50 mM 0.0389 mL 0.1947 mL 0.3895 mL 0.9737 mL
60 mM 0.0325 mL 0.1623 mL 0.3246 mL 0.8114 mL
80 mM 0.0243 mL 0.1217 mL 0.2434 mL 0.6086 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Loperamide hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Loperamide34552-83-5R-18553R18553R 18553Opioid ReceptorAutophagyInhibitorinhibitorinhibit

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