Loperamide
Based on 13 publication(s) in Google Scholar
Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with Ki 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.85%
- No. CAS: 53179-11-6
- Fòrmula: C29H33ClN2O2
- Peso molecular:477.04
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Loperamide
More- Nature. 2025 Dec;648(8094):755-763. [Abstract]
- Phytomedicine. 2025 Nov 25:148:157417. [Abstract]
- J Transl Med. 2021 Jul 23;19(1):317. [Abstract]
- Int J Biol Macromol. 2026 Apr:357:151532. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- eFood. 2025 Jul 14.
- Food Qual Saf. 2024 Sep 10.
- Oncol Rep. 2025 Oct;54(4):133. [Abstract]
- Viruses. 2021 Jun 28;13(7):1255. [Abstract]
- Neurogastroenterol Motil. 2026 Apr;38(4):e70298. [Abstract]
- Dig Dis Sci. 2025 Nov 15. [Abstract]
- J Appl Microbiol. 2023 Aug 1;134(8):lxad153. [Abstract]
- Curr Med Sci. 2025 Aug 29. [Abstract]
Ver todos los productos específicos de isoformas Opioid Receptor
More
Actividad biológica
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μ Opioid Receptor/MOR 3 () |
δ Opioid Receptor/DOR 48 () |
κ Opioid Receptor/KOR 1156 () |
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | IC50 |
2.5 μM
Compound: Loperamide
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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
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[PMID: 11964599] |
| CHO | EC50 |
156 nM
Compound: Loperamide
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Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
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[PMID: 15456245] |
| CHO | EC50 |
58 nM
Compound: Loperamide
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Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes
Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes
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[PMID: 15456245] |
| HEK293 | IC50 |
23.7 μM
Compound: loperamide
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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
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[PMID: 18788725] |
| Vero | CC50 |
29.26 μM
Compound: Loperamide
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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
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
9.27 μM
Compound: Loperamide
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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
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10.1101/2020.03.20.999730 |
Loperamide exhibits potent, selective affinity for cloned human μ opioid receptors (Ki = 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.
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.
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Animal Model:Sprague-Dawley with knee joint (male)[1]
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Dosage:0.3 mg
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Administration:intra-articular injection
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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.
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Animal Model:Prostaglandin E2-induced Wistar (male, 220-280g, fasted overnight with ad libitum water access)[2]
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Dosage:4 mg/kg
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Administration:i.g.; single dose
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 53179-11-6
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Appearance Solid
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Peso molecular 477.04
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Fòrmula C29H33ClN2O2
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Color White to off-white
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SMILES
O=C(C(C1=CC=CC=C1)(CCN2CCC(C3=CC=C(C=C3)Cl)(CC2)O)C4=CC=CC=C4)N(C)C
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Synonyms
ADL 2-1294
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Journal Impact Factor
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Most Recent
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Nature
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 Nov 25:148:157417. 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 -
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Oncol Rep
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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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.
| 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
HY-156131 Related Classifications
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