Ivermectin

Synonyms: MK-933

Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.

Ivermectin Chemical Structure

Ivermectin Chemical Structure

CAS No. 70288-86-7

Purity & Quality Control

Ivermectin Related Products

Biological Activity

Description Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
Targets
chloride channel [3]
In vitro
In vitro

Ivermectin has potent antiviral activity towards both HIV-1 anddengue virus, both of which are strongly reliant on importin α/β nuclear import, with respect to the HIV-1 integrase and NS5 (non-structural protein 5) polymerase proteins respectively. [1] Ivermectin binds to a novel site on the GABAA receptor and allosterically enhances the affinity of the GABA binding site in mouse hippocampal embryonic neurons. [2] Ivermectin disrupts neurotransmission processes regulated by GluCl activity by binding to nematode glutamate-gated chloride channels (GluCls). Ivermectin decreases the amount of protein released from microfilariae. [3]

Experimental Result Images Methods Biomarkers Images PMID
Western blot YAP1 / CTGF 29296196
Immunofluorescence YAP1 29296196
Growth inhibition assay Cell viability 29296196
In Vivo
In vivo

Ivermectin (1.25-10 mg/kg, intraperitoneal) significantly reduces 24-h alcohol consumption and intermittent limited access (4-hours) binge drinking, and operant alcohol self-administration (1-h). Ivermectin also produces a significant reduction in 24-h saccharin consumption, but does not alter operant sucrose self-administration. [4] Ivermectin improves mouse survival rate induced by a lethal dose of LPS. Ivermectin significantly decreases the production of TNF-alpha, IL-1ss and IL-6 in vivo and in vitro. Ivermectin suppresses NF-kB translocation induced by LPS. [5]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06404333 Not yet recruiting
Scabies
University of Oxford|Fundação de Medicina Tropical Dr. Heitor Vieira Dourado|Fundação de Dermatologia Tropical e Venereologia Alfredo da Matta (FUAM)|University of Basel|ClinSearch
October 1 2024 Phase 2
NCT05500326 Not yet recruiting
Scabies; Itch|Scabies
Murdoch Childrens Research Institute|Burnet Institute|Lao Tropical and Public Health Institute
June 2024 Phase 2
NCT06373835 Not yet recruiting
Strongyloides Stercoralis Infection|Strongyloidiasis
Swiss Tropical & Public Health Institute|National Institute of Public Health Vientiane Laos
May 1 2024 Phase 2
NCT06332872 Active not recruiting
Pediculus Capitis Infestation|Permethrin Adverse Reaction|Dimethicone Adverse Reaction|Permethrin Allergy|Dimethicone Allergy|Ivermectin|School-age Children
Phramongkutklao College of Medicine and Hospital
December 15 2023 Phase 4

Chemical Information & Solubility

Molecular Weight 875.09 Formula

C48H74O14

CAS No. 70288-86-7 SDF Download Ivermectin SDF
Smiles CCC(C)C1C(CCC2(O1)CC3CC(O2)CC=C(C(C(C=CC=C4COC5C4(C(C=C(C5O)C)C(=O)O3)O)C)OC6CC(C(C(O6)C)OC7CC(C(C(O7)C)O)OC)OC)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 175 mg/mL ( (199.97 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 28 mg/mL

Water : Insoluble


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In vivo
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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.

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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.

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Frequently Asked Questions

Question 1:
I would like to use S1351 for in vivo studies via IP injection? Do you have some suggestions?

Answer:
You could use the following formula for working solution: 5%DMSO + 40%PEG300 + 5% Tween + ddH2O, reaching a concentration of 12.5mg/ml.

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