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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.
|Formula||C48H74O14 (B1a form)|
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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.
|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|
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.
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
Citations are publications that use Tocris products. Selected citations for Ivermectin include:
Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590
Fischer et al (2013) Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal 10 313 PMID: 24163006
Dhuna et al (2019) Ginsenosides Act As Positive Modulators of P2X4 Receptors. Mol Pharmacol 95 210 PMID: 30545933
Ren et al (2016) A biofidelic 3D culture model to study the development of brain cellular systems. Pharmacol Res Perspect 6 24953 PMID: 27112667
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
Do you know of a great paper that uses Ivermectin from Tocris? Please let us know.
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Potentiates P2X4 responses in cultured microglia
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.