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/ Ivermectin/伊维菌素

Ivermectin/伊维菌素 {[allProObj[0].p_purity_real_show]}

货号：A292838 同义名： 伊维茵素 / MK-933; 22,23-dihydro Avermectin B1

Ivermectin是一种广谱抗寄生虫药，通过激活氯离子通道和抑制核导入，具有强大的抗病毒活性，包括对 HIV-1、登革热病毒等的抑制作用。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Ivermectin/伊维菌素 化学结构 CAS号：70288-86-7
Ivermectin/伊维菌素 化学结构
CAS号：70288-86-7
Ivermectin/伊维菌素 3D分子结构
CAS号：70288-86-7
Ivermectin/伊维菌素 化学结构 CAS号：70288-86-7
Ivermectin/伊维菌素 3D分子结构 CAS号：70288-86-7
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Ivermectin/伊维菌素 纯度/质量文件 产品仅供科研

货号：A292838 标准纯度： {[allProObj[0].p_purity_real_show]}
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Ivermectin/伊维菌素 生物活性

描述 Ivermectin (IVM), a widely used antiparasitic agent in human and veterinary medicine. Ivermectin (MK-933) activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis[3]. Ivermectin is a specific positive allosteric effector of heterologously expressed P2X(4) and possibly of heteromeric P2X(4)/P2X(6) channels. In the submicromolar range (EC50 = 250 nM) the action of Ivermectin is rapid and reversible, resulting in increased amplitude and slowed deactivation of P2X4 channel currents evoked by ATP. Ivermectin also markedly increased the potency of ATP and that of the normally low-potency agonist alpha, beta-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X(4) channels[4]. Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus, both of which are strongly reliant on importin α/β nuclear import, with respect to the HIV-1 integrase and NS5 (non-structural protein 5) polymerase proteins respectively. Ivermectin strongly inhibits the binding of Impα/β1 to NS5 (IC50 = 17 μM), but not of Impβ1 alone to NS5[5]. Ivermectin also inhibits bovine herpesvirus 1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import[6].

Ivermectin/伊维菌素 细胞实验

Cell Line
Concentration Treated Time Description References
Xenopus oocytes 30 µM 10 minutes Study the desensitization effect of ivermectin on α7nAChR TMD+ICD channels ACS Chem Neurosci. 2023 Mar 15;14(6):1156-1165.
RT4 cells 26.7 µM (24h, IC50), 14.9 µM (48h, IC50), 10.0 µM (72h, IC50) 24, 48, 72 hours Ivermectin inhibited RT4 cell proliferation, induced G1 phase cell cycle arrest and caspase-dependent apoptosis, mediated via JNK signaling pathway. Int J Med Sci. 2022 Sep 11;19(10):1567-1575.
T24 cells 26.7 µM (24h, IC50), 14.9 µM (48h, IC50), 10.0 µM (72h, IC50) 24, 48, 72 hours Ivermectin inhibited T24 cell proliferation, induced G1 phase cell cycle arrest and caspase-dependent apoptosis. Int J Med Sci. 2022 Sep 11;19(10):1567-1575.
RT4 cells 26.7 µM (24h), 14.9 µM (48h), 10.0 µM (72h) 24, 48, 72 hours Ivermectin inhibited RT4 cell proliferation, induced G1 phase cell cycle arrest and caspase-dependent apoptosis, mediated via JNK signaling pathway. Int J Med Sci. 2022 Sep 11;19(10):1567-1575.
T24 cells 20.5 µM (24h), 17.4 µM (48h), 16.6 µM (72h) 24, 48, 72 hours Ivermectin inhibited T24 cell proliferation, induced G1 phase cell cycle arrest and caspase-dependent apoptosis. Int J Med Sci. 2022 Sep 11;19(10):1567-1575.
SARS-CoV-2-infected cell lines 5 µM 48 hours To evaluate the inhibitory effect of ivermectin on SARS-CoV-2 replication, results showed inhibition of viral replication within 48 hours at a concentration of 5 μM Geroscience. 2023 Aug;45(4):2179-2193.
CFSC cells (a rat HSC cell line) 3 µM, 6 µM 48 hours To investigate whether ivermectin could directly regulate HSC activation. Ivermectin pretreatment dose-dependently reduced the TGF-β1-induced elevation of α-SMA protein levels, revealing that ivermectin could suppress TGF-β1-induced HSC activation in vitro. Int J Mol Sci. 2022 Dec 16;23(24):16043.
CFSC cells (a rat HSC cell line) 3 µM, 6 µM, 12 µM, 25 µM 48 hours To assess the cytotoxic effects of ivermectin on HSCs. Low-dose ivermectin (3 and 6 μM) had no significant effect on cell survival, whereas high-dose (12 and 25 μM) obviously reduced cell viability. Int J Mol Sci. 2022 Dec 16;23(24):16043.
Plasmodium falciparum laboratory strains and isolates 0.02 to 10 µM 72 hours To evaluate the antimalarial activity of ivermectin and its metabolites against asexual blood stage Plasmodium falciparum. Results showed that the mean IC50 of ivermectin parent compound was 0.81 μM, and the metabolites were 2-fold to 4-fold less active than the parent compound. Antimicrob Agents Chemother. 2023 Jul 18;67(7):e0173022.
MCF-7 cells 15 µM 18 hours Nabumetone was confirmed as a novel activator of ERα. Chem Res Toxicol. 2021 Feb 15;34(2):313-329
Aeromonas taiwanensis ZJB-18,044 50 mg/L 5 d To evaluate the degradation ability of strain ZJB-18,044 towards Doramectin, results showed that the strain can efficiently degrade Doramectin. Biodegradation. 2020 Dec;31(4-6):275-288

Ivermectin/伊维菌素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c male mice CCl4-induced liver fibrosis model Intraperitoneal injection 1.3 mg/kg Daily injections for 4 weeks To evaluate the protective effects of ivermectin on liver fibrosis. Ivermectin alleviated CCl4-induced histopathological changes, improved liver function, reduced collagen deposition, and downregulated the expression of profibrotic genes. Additionally, ivermectin inhibited intrahepatic macrophage accumulation and suppressed the production of proinflammatory factors. Int J Mol Sci. 2022 Dec 16;23(24):16043.

Ivermectin/伊维菌素 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00342576 - Completed - India ... 展开 >> Tuberculosis Research Centre Chennai, India 收起 <<
NCT02644525 Loaisis Phase 2 Not yet recruiting June 30, 2019 Cameroon ... 展开 >> Centre de Recherche sur les Filarioses et Autres Maladies Tropicales Not yet recruiting Mbalmayo, Cameroon Contact: Joseph Kamgno, M.D.    Not Listed    kamgno@crfilmt.org 收起 <<
NCT01080989 Flavivirus Infection ... 展开 >> Alphavirus Infections Malaria Parasitic Disease Leptospirosis Hypertension Metabolic Syndromes 收起 << Not Applicable Completed - Taiwan ... 展开 >> Kaoshing Medical University Chung-Ho Memorial Hospital Kaoshiung, Taiwan 收起 <<

Ivermectin/伊维菌素 参考文献

[1]Wagstaff KM, Sivakumaran H, et al. Ivermectin is a specific inhibitor of importin α/β-mediated nuclear import able to inhibit replication of HIV-1 and dengue virus. Biochem J. 2012 May 1;443(3):851-6.

[2]Reiter RJ. Oxidative damage in the central nervous system: protection by melatonin. Prog Neurobiol. 1998 Oct;56(3):359-84.

[3]Priel A, Silberberg SD. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004;123(3):281-293

[4]Khakh BS, Proctor WR, Dunwiddie TV, Labarca C, Lester HA. Allosteric control of gating and kinetics at P2X(4) receptor channels. J Neurosci. 1999;19(17):7289-7299

[5]Wagstaff KM, Sivakumaran H, Heaton SM, Harrich D, Jans DA. Ivermectin is a specific inhibitor of importin α/β-mediated nuclear import able to inhibit replication of HIV-1 and dengue virus. Biochem J. 2012;443(3):851-856

[6]Raza S, Shahin F, Zhai W, et al. Ivermectin Inhibits Bovine Herpesvirus 1 DNA Polymerase Nuclear Import and Interferes with Viral Replication. Microorganisms. 2020;8(3):409. Published 2020 Mar 13

Ivermectin/伊维菌素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.71mL

1.14mL

0.57mL

11.43mL

2.29mL

1.14mL

Ivermectin/伊维菌素 技术信息

CAS号70288-86-7
分子式C48H74O14
分子量 875.09
SMILES Code 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
MDL No. MFCD00869511
别名 伊维茵素 ;MK-933; 22,23-dihydro Avermectin B1; Pandex; Noromectin; MK-0933; 1 Mectizan; L 64047; Ivomec; CD-5024; K-237
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 250 mg/mL，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Ivermectin/伊维菌素 |Ivermectin/伊维菌素 | 伊维茵素 | MK-933 | 22,23-dihydro Avermectin B1 | Pandex | Noromectin | MK-0933 | 1 Mectizan | L 64047 | Ivomec | CD-5024 | K-237 | 70288-86-7 | 驱虫剂 | Antiparasitic | 糖类 | Ivermectin/伊维菌素 纯度/质量文件 | Ivermectin/伊维菌素 生物活性 | Ivermectin/伊维菌素 临床数据 | Ivermectin/伊维菌素 参考文献 | Ivermectin/伊维菌素 实验方案 | Ivermectin/伊维菌素 技术信息

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