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Submit ReviewIvermectin
Description: Positive allosteric modulator of α7 nAChRs; also positive allosteric modulator of P2X4 receptors
Chemical Name: 22,23-Dihydroavermectin B1
Purity: ≥96% (HPLC)
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 |
| InChI Key | AZSNMRSAGSSBNP-XPNPUAGNSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50 |
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.
| 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 |
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Product Datasheets for Ivermectin
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:
Ren et al (2016) A biofidelic 3D culture model to study the development of brain cellular systems. Pharmacol Res Perspect 6 24953 PMID: 27112667
Dhuna et al (2019) Ginsenosides Act As Positive Modulators of P2X4 Receptors. Mol Pharmacol 95 210 PMID: 30545933
Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590
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
Fischer et al (2013) Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal 10 313 PMID: 24163006
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!
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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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