Loperamide (Synonyms: ADL 2-1294)

Name: Loperamide
Brand: MedChemExpress
SKU: HY-156131
Rating: 5.0 (12 reviews)

Cat. No.: HY-156131 Purity: 99.85%: Data Sheet
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Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with K_i valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE₂(HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea.

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

Loperamide Chemical Structure

CAS No. : 53179-11-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Loperamide:

Loperamide-d₆ In-stock
Loperamide hydrochloride In-stock

12 Publications Citing Use of MCE Loperamide

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•Related Small Molecules:

•Related Proteins:

View All Opioid Receptor Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

μ Opioid Receptor/MOR

3 ()

δ Opioid Receptor/DOR

48 ()

κ Opioid Receptor/KOR

1156 ()

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	156 nM Compound: Loperamide	Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes	[PMID: 15456245]
CHO	EC₅₀	58 nM Compound: Loperamide	Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes	[PMID: 15456245]
Caco-2	IC₅₀	2.5 μM Compound: Loperamide	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	[PMID: 11964599]
HEK293	IC₅₀	23.7 μM Compound: loperamide	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
Vero	CC₅₀	29.26 μM Compound: Loperamide	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	9.27 μM Compound: Loperamide	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Loperamide exhibits potent, selective affinity for cloned human μ opioid receptors (K_i = 3.3 nM) and acts as a functional agonist at these receptors in transfected CHO cells, with an EC₅₀ of 56 nM for [³⁵S]GTPγS binding stimulation and an IC₅₀ of 25 nM for Forskolin (HY-15371)-stimulated cAMP accumulation inhibition^[1].

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

In Vivo

Loperamide (0.3 mg; intra-articular injection) administered locally into an inflamed rat knee joint produces potent, naloxone-reversible antinociception to knee compression, with no effect when administered to a non-inflamed joint or intramuscularly^[1].
Loperamide (local intrapaw injection) administered intrapaw potently inhibits late-phase Forskolin (HY-15371)-induced flinching in rats (A₅₀ = 6 μg), with no effect on early-phase flinching or when delivered to a non-inflamed contralateral paw^[1].
Loperamide (local intrapaw injection) administered locally into a CFA (HY-153808)-inflamed rat paw produces antinociception via increased paw pressure thresholds (ED₅₀ = 21 μg)^[1].
Loperamide (local intrapaw injection) administered locally into a tape stripping-inflamed rat paw produces antinociception via increased paw pressure thresholds (ED₅₀ = 71 μg)^[1].
Loperamide (4 mg/kg; i.g.; single dose) enhances baseline intestinal absorption of water, electrolytes, and glucose, and reverses Prostaglandin E₂(HY-101952)-induced intestinal hypersecretion in male Wistar rats^[2].
Loperamide (4 mg/kg; i.g.; single dose) reverses Cholera toxin (HY-P1446)-induced intestinal hypersecretion in male Wistar rats without altering cholera toxin-mediated elevations in adenylate cyclase activity or tissue cAMP levels^[2].

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

Animal Model:	Sprague-Dawley with knee joint (male)^[1]
Dosage:	0.3 mg
Administration:	intra-articular injection
Result:	Produced potent antinociception to knee compression. Had its antinociceptive effect antagonized by Naloxone (HY-17417A). Failed to inhibit compression-induced changes in blood pressure when injected into the contralateral non-inflamed knee joint or via intramuscular route.

Animal Model:	Prostaglandin E₂-induced Wistar (male, 220-280g, fasted overnight with ad libitum water access)^[2]
Dosage:	4 mg/kg
Administration:	i.g.; single dose
Result:	Enhanced net absorption rates of water (+40.1 μl/min/g wet weight of gut), sodium (+6.3 μmol/min/g), chloride (+5.3 μmol/min/g), and glucose (+0.40 μmol/min/g). Reversed PGE₂-induced secretion of water, sodium, and chloride to net absorption. Reduced PGE₂-induced potassium secretion.

Clinical Trial

Molecular Weight

477.04

Formula

C₂₉H₃₃ClN₂O₂

CAS No.

53179-11-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C1=CC=CC=C1)(CCN2CCC(C3=CC=C(C=C3)Cl)(CC2)O)C4=CC=CC=C4)N(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (209.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0963 mL	10.4813 mL	20.9626 mL
5 mM	0.4193 mL	2.0963 mL	4.1925 mL
10 mM	0.2096 mL	1.0481 mL	2.0963 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.85%

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Data Sheet (279 KB) SDS (393 KB)

COA (251 KB) HNMR (295 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. DeHaven-Hudkins D L, et al. Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity[J]. The Journal of pharmacology and experimental therapeutics, 1999, 289(1): 494-502.

[2]. Sandhu BK, et al. Loperamide: studies on its mechanism of action. Gut. 1981;22(8):658-662. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0963 mL	10.4813 mL	20.9626 mL	52.4065 mL
	5 mM	0.4193 mL	2.0963 mL	4.1925 mL	10.4813 mL
	10 mM	0.2096 mL	1.0481 mL	2.0963 mL	5.2407 mL
	15 mM	0.1398 mL	0.6988 mL	1.3975 mL	3.4938 mL
	20 mM	0.1048 mL	0.5241 mL	1.0481 mL	2.6203 mL
	25 mM	0.0839 mL	0.4193 mL	0.8385 mL	2.0963 mL
	30 mM	0.0699 mL	0.3494 mL	0.6988 mL	1.7469 mL
	40 mM	0.0524 mL	0.2620 mL	0.5241 mL	1.3102 mL
	50 mM	0.0419 mL	0.2096 mL	0.4193 mL	1.0481 mL
	60 mM	0.0349 mL	0.1747 mL	0.3494 mL	0.8734 mL
	80 mM	0.0262 mL	0.1310 mL	0.2620 mL	0.6551 mL
	100 mM	0.0210 mL	0.1048 mL	0.2096 mL	0.5241 mL

Loperamide Related Classifications

Neurological Disease Inflammation/Immunology

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:

Loperamide53179-11-6ADL 2-1294Opioid ReceptorCHO cellshuman μ opioid receptorPGE2cholera toxinprotracted diarrhoeaFreund's adjuvantforskolininflammatory paincAMPnaloxoneInhibitorinhibitorinhibit

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Loperamide (Synonyms: ADL 2-1294)

Customer Review

Other Forms of Loperamide:

Loperamide Related Antibodies

12 Publications Citing Use of MCE Loperamide

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Opioid Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Loperamide Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Loperamide Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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