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Description: Positive allosteric modulator of α7 nAChRs; also positive allosteric modulator of P2X4 receptors
Chemical Name: 22,23-Dihydroavermectin B1
Purity: ≥96% (HPLC)
Citations (5)
Reviews (1)
Literature (2)

Biological Activity for Ivermectin

Ivermectin is a positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor and the purinergic P2X4 receptor. Antihelmintic and antiviral. Also modulates glutamate- and GABA-activated chloride channels. Potentiates glycine-gated currents at low concentrations (30 nM). Inhibits replication of SARS-CoV-2 in vitro (IC50 ~ 2μM).

This product is composed of both Ivermectin B1a (>90%) and Ivermectin B1b.

Technical Data for Ivermectin

M. Wt 875.1
Formula C48H74O14 (B1a form)
Storage Desiccate at +4°C
Purity ≥96% (HPLC)
CAS Number 70288-86-7
PubChem ID 6321424
Smiles O[C@H]1[C@H](C)O[C@](O[C@H]2[C@@H](O[C@](O[C@H](/C(C)=C/C[C@@]4([H])O[C@@]7(CC[C@H](C)[C@@]([H])([C@]([H])(C)C)O7)C[C@@H]6C4)[C@@H](C)/C=C/C=C3/[C@]5(O)[C@]([C@H](O)C(C)=CC5C(O6)=O)([H])OC3)([H])C[C@@H]2OC)C)([H])C[C@@H]1OC.O[C@H]8[C@H](C)O[C@](O[C@H]9[C@@H](O[C@](O[C@H](/C(C)=C/C[C@@]%11([H])O[C@@]%14(CC[C@H](C)[C@@]([H])([C@]([H])(C)CC)O%14)C[C@@H]%13C%11)[C@@H](C)/C=C/C=C%10/[C@]%12(O)[C@]([C@H](O)C(C)=CC%12C(O%13)=O)([H])OC%10)([H])C[C@@H]9OC)C)([H])C[C@@H]8OC

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Ivermectin

Solvent Max Conc. mg/mL Max Conc. mM

Preparing Stock Solutions for Ivermectin

The following data is based on the product molecular weight 875.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.29 mL 11.43 mL 22.85 mL
2.5 mM 0.46 mL 2.29 mL 4.57 mL
5 mM 0.23 mL 1.14 mL 2.29 mL
25 mM 0.05 mL 0.23 mL 0.46 mL

Molarity Calculator

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References for Ivermectin

References are publications that support the biological activity of the product.

Adelsberger et al (2000) Activation of rat recombinant α1β2γ2S GABAA receptor by the insecticide iverm. Eur.J.Pharmacol. 394 163 PMID: 10771281

Khakh et al (1999) Allosteric control of gating and kinetics at P2X4 receptor channels. J.Neurosci. 19 7289 PMID: 10460235

Krause et al (1998) Ivermectin: a positive allosteric effector of the α7 neuronal nicotinic acetylcholine receptor. Mol.Pharmacol. 53 283 PMID: 9463487

Shan et al (2001) Ivermectin, an unconventional agonist of the glycine receptor chloride channel. J.Biol.Chem. 276 12556 PMID: 11278873

Merck Index 12 5264

Caly et al (2020) The FDA-approved drug ivermectin inhibits the replication of SARS-CoV-2 in vitro. Antiviral Res. 178 PMID: 32251768

If you know of a relevant reference for Ivermectin, please let us know.

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Keywords: Ivermectin, Ivermectin supplier, Allosteric, modulators, α7, alpha7, nicotinic, receptors, Positive, allosteric, P2X4, Acetylcholine, nAChR, Purinergic, purinoceptors, PAM, SARS-CoV-2, COVID-19, antiviral, antiparasitic, P2X, Receptors, Nicotinic, (a7), Coronavirus, 1260, Tocris Bioscience

5 Citations for Ivermectin

Citations are publications that use Tocris products. Selected citations for Ivermectin include:

Dhuna et al (2019) Ginsenosides Act As Positive Modulators of P2X4 Receptors. Mol Pharmacol 95 210 PMID: 30545933

Fischer et al (2013) Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal 10 313 PMID: 24163006

Dolma et al (2016) Inhibition of Dopamine Receptor D4 Impedes Autophagic Flux, Proliferation, and Survival of Glioblastoma Stem Cells. Cancer Cell 29 859 PMID: 27300435

Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590

Ren et al (2016) A biofidelic 3D culture model to study the development of brain cellular systems. Pharmacol Res Perspect 6 24953 PMID: 27112667

Do you know of a great paper that uses Ivermectin from Tocris? Please let us know.

Reviews for Ivermectin

Average Rating: 5 (Based on 1 Review.)

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P2X4 potentiation.
By Anonymous on 10/02/2018
Assay Type: In Vitro
Species: Mouse

Potentiates P2X4 responses in cultured microglia

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Nicotinic ACh Receptors Scientific Review

Nicotinic ACh Receptors Scientific Review

Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.

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Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.