Cat. No.: HY-156131

Loperamide

(Synonyms: ADL 2-1294)

13 Cited Publications

Customer Review

Based on 13 publication(s) in Google Scholar

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.

Purity: 99.85%
CAS No.: 53179-11-6
Formula: C₂₉H₃₃ClN₂O₂
Molecular Weight:477.04

Storage:

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

Loperamide Chemical Structure

CAS No.: 53179-11-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

μ Opioid Receptor/MOR

3 ()

δ Opioid Receptor/DOR

48 ()

κ Opioid Receptor/KOR

1156 ()

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 53179-11-6
Appearance Solid
Molecular Weight 477.04
Formula C₂₉H₃₃ClN₂O₂
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
Synonyms

ADL 2-1294
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

Publications (13)

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Nature

Structural snapshots capture nucleotide release at the μ-opioid receptor. [Abstract]

2025 Dec;648(8094):755-763. PMID: 41193810
Phytomedicine

Xiaoer Qixing Cha alleviates functional constipation via regulating gut microbiota and short-chain fatty acids in mice. [Abstract]

2025 Oct 16:148:157417. PMID: 41161186
J Transl Med

Constipation induced gut microbiota dysbiosis exacerbates experimental autoimmune encephalomyelitis in C57BL/6 mice. [Abstract]

2021 Jul 23;19(1):317. PMID: 34301274
Int J Biol Macromol

L-β-Galactoglucan alleviates loperamide-induced constipation in mice and regulates gut microbiota and metabolism. [Abstract]

2026 Apr:357:151532. PMID: 41887441
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
eFood

2025 Jul 14.
Food Qual Saf

2024 Sep 10.
Oncol Rep

Loperamide reverses 5‑FU resistance in colorectal cancer by activating autophagy. [Abstract]

2025 Oct;54(4):133. PMID: 40776759
Viruses

Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]

2021 Jun 28;13(7):1255. PMID: 34203149
Neurogastroenterol Motil

Acacetin Alleviates Loperamide-Induced Functional Constipation by Inhibiting P53-Mediated Apoptosis in Colonic Epithelial Cells. [Abstract]

2026 Apr;38(4):e70298. PMID: 41913080
Dig Dis Sci

Kaempferol Ameliorates Functional Constipation in Mice by Regulating Autophagy of Interstitial Cells of Cajal via the p53/AMPK/mTOR Axis. [Abstract]

2025 Nov 15. PMID: 41240265
J Appl Microbiol

Houpo Paiqi Mixture Promotes Intestinal Motility in Constipated Rats by Modulating Gut Microbiota and Activating 5-HT-cAMP-PKA Signal Pathway. [Abstract]

2023 Aug 1;134(8):lxad153. PMID: 37481692
Curr Med Sci

Konjac Oligosaccharide Alleviates Constipation in Mice via 5-HT4R/cAMP/PKA/p-CREB Pathway Activation. [Abstract]

2025 Aug 29. PMID: 40879997

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

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Loperamide

Publications Citing Use of MedChemExpress (MCE) Loperamide

All Opioid Receptor Isoforms

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Loperamide Related Classifications

HY-156131 Related Classifications