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Submit ReviewIvermectin 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.
分子量 | 875.1 |
公式 | C48H74O14 (B1a form) |
储存 | Desiccate at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 Ivermectin 的部分引用包括:
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
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
Fischer et al (2013) Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal 10 313 PMID: 24163006
Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590
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Potentiates P2X4 responses in cultured microglia