Ivermectin (MK-933)

Catalog No.S1351

For research use only.

Ivermectin (MK-933, IVM) 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 has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.

Ivermectin (MK-933) Chemical Structure

CAS No. 70288-86-7

Selleck's Ivermectin (MK-933) has been cited by 9 Publications

Purity & Quality Control

Choose Selective Chloride Channel Inhibitors

Biological Activity

Description Ivermectin (MK-933, IVM) 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 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

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]

Assay
Methods Test Index PMID
Western blot YAP1 / CTGF 29296196
Immunofluorescence YAP1 29296196
Growth inhibition assay Cell viability 29296196
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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(114.27 mM)
Water Insoluble
Ethanol ''28 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 875.09
Formula

C48H74O14

CAS No. 70288-86-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05004571 Recruiting Drug: EQU-001|Drug: Placebo Safety Issues Equilibre Biopharmaceuticals July 6 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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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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