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My CartCAS：70288-86-7
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 70288-86-7 |
| Name | Ivermectin |
| Molecular Formula | C48H74O14 |
| Molecular Weight | 875.11 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 274-536-0 |
| SMILES | CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@H](/C(C)=C/C[C@@H]3C[C@H]4C[C@@]5(O[C@]([H])(C(C)C)[C@@H](C)CC5)O3)[C@@H](C)/C=C/C=C6CO[C@@]7([H])[C@]\6(O)[C@H](C(O4)=O)C=C(C)[C@H]7O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O.CO[C@H]8C[C@H](O[C@H]9[C@H](C)O[C@@H](O[C@H](/C(C)=C/C[C@@H]%10C[C@H]%11C[C@@]%12(O[C@]([H])([C@@H](C)CC)[C@@H](C)CC%12)O%10)[C@@H](C)/C=C/C=C%13CO[C@@]%14([H])[C@]\%13(O)[C@H](C(O%11)=O)C=C(C)[C@H]%14O)C[C@@H]9OC)O[C@@H](C)[C@@H]8O |
| InChIKey | AZSNMRSAGSSBNP-XPNPUAGNSA-N |
| InChI | InChI=1S/C48H74O14/c1-11-25(2)43-28(5)17-18-47(62-43)23-34-20-33(61-47)16-15-27(4)42(26(3)13-12-14-32-24-55-45-40(49)29(6)19-35(46(51)58-34)48(32,45)52)59-39-22-37(54-10)44(31(8)57-39)60-38-21-36(53-9)41(50)30(7)56-38/h12-15,19,25-26,28,30-31,33-45,49-50,52H,11,16-18,20-24H2,1-10H3/b13-12+,27-15+,32-14+/t25-,26-,28-,30-,31-,33+,34-,35-,36-,37-,38-,39-,40+,41-,42-,43+,44-,45+,47+,48+/m0/s1 |
| PubChem CID | 6321424 |
| Target Point | Parasite;HIV;Mitophagy;HSV;SARS-CoV |
| Passage | Anti-infection |
| Background | Ivermectin is a broad-spectrum antiparasitic compound with anti-HIV-1, SARS-CoV-2 and dengue virus activities. Ivermectin is a specific Imp α/β 1-mediated nuclear induction inhibitors and P2X4 and α 7 nAChRs, a positive isomeric effector. |
| Biological Activity | Ivermectin是广泛使用于人类和动物的抗寄生虫剂。它是P2X4和α7 nAChRs的正异构效应物。[1-4] |
| In Vitro | 伊维菌素(IVM)是异源表达的P2X4和可能的异聚P2X4 / P2X6通道的特异性正变构效应子。在亚微摩尔范围内(EC50 = 250nM)，IVM的作用是快速且可逆的，导致由ATP引起的P2X4通道电流的振幅增加和减慢的失活。在不改变P2X4通道的离子选择性的情况下，IVM还显着增加ATP和正常低效激动剂a，b-亚甲基-ATP的效力，而不改变P2X4通道的离子选择性[1]。 IVM激活寄生虫神经和肌肉中的谷氨酸门控氯通道，导致膜超极化和肌肉麻痹。 IVM的主要作用方式很可能是破坏寄生虫的摄食活动，导致饥饿[2]。在微摩尔范围内预先施用伊维菌素可强烈增强随后在非洲爪蟾卵母细胞和K-28细胞中重建的神经元鸡或人α7烟碱乙酰胆碱受体的乙酰胆碱诱发电流[3]。伊维菌素激活大鼠重组α1β2γ2sGABAA受体。用10mM GABA激活通道导致电流在1ms内上升至其最大振幅。 GABA的EC50值为7.5μM[4]。 |
| Data Literature Source | [1]. Khakh BS， et al. Allosteric control of gating and kinetics at P2X (4) receptor channels. J Neurosci. 1999 Sep 1; 19 (17) :7289-99. [2]. Priel A， et al. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004 Mar; 123 (3) :281-93. [3]. Krause RM， et al. Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor. Mol Pharmacol. 1998 Feb; 53 (2) :283-94. [4]. Adelsberger H， et al. Activation of rat recombinant alpha (1) beta (2) gamma (2S) GABA (A) receptor by the insecticide ivermectin. Eur J Pharmacol. 2000 Apr 14; 394 (2-3) :163-70. |
| Unit | Bottle |
| Specification | 100mg 10mM*1mL in DMSO 500mg |
Ivermectin is a broad-spectrum antiparasitic compound. Ivermectin can induce autophagy through the AKT/mTOR signaling pathway and induce mitochondrial autophagy. Ivermectin is a specific Impα/ β1-mediated nucleotophoresis inhibitor with strong antiviral activity against both HIV-1 and dengue viruses. Ivermectin is also a positive effector of P2X4 and α7 nAChRs. Ivermectin has been reported to have anti-SARS-CoV-2 /COVID-19 potential.
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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