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/ Atovaquone/阿托伐醌

Atovaquone/阿托伐醌 {[allProObj[0].p_purity_real_show]}

货号：A242112 同义名： Atavaquone; BW 566C

Atovaquone is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.

Atovaquone/阿托伐醌 化学结构 CAS号：95233-18-4
Atovaquone/阿托伐醌 化学结构
CAS号：95233-18-4
Atovaquone/阿托伐醌 3D分子结构
CAS号：95233-18-4
Atovaquone/阿托伐醌 化学结构 CAS号：95233-18-4
Atovaquone/阿托伐醌 3D分子结构 CAS号：95233-18-4
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Atovaquone/阿托伐醌 纯度/质量文件 产品仅供科研

货号：A242112 标准纯度： {[allProObj[0].p_purity_real_show]}
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Atovaquone/阿托伐醌 生物活性

描述 Atovaquone is a powerful suppressor of protozoan parasites with a broad-spectrum activity, but an extremely low water solubility and bioavailability. Oral administration of atovaquone nanoemulsion increased oral bioavailability, tissue distribution and mice survival time and reduced parasitemia and number and size of the brain cysts[3]. While atovaquone has potent in vitro activity against Toxoplasma gondii, it is poorly absorbed after oral administration and shows poor therapeutic efficacy against TE(toxoplasma encephalitis). Development of TE and mortality in mice treated with 1.0- or 0.1-mg/kg i.v. doses of ANS (atovaquone nanosuspensions) did not differ from that in mice treated orally with 100 mg of atovaquone/kg[4]. Atovaquone, an antiprotozoal and antipneumocystic agent, is predominantly cleared by biliary excretion of unchanged parent drug[5]. Atovaquone potently inhibits the propagation of MCF7-derived CSCs, with an IC-50 of 1 μM, as measured using the mammosphere assay. In addition to targeting the proliferation of CSCs (Cancer Stem-like Cells), atovaquone also induces apoptosis in both CD44+/CD24low/- CSC and ALDH+ CSC populations, during exposure to anchorage-independent conditions for 12 hours[6].

Atovaquone/阿托伐醌 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
NCT03163121 Malaria Phase 1 Recruiting October 2018 Netherlands ... 展开 >> Leiden University Medical Center, Albinusdreef 2 Recruiting Leiden, Netherlands, 2333 ZA Contact: Leo G. Visser, MD    31715266354    l.g.visser@lumc.nl    Contact: Meta Roestenberg, MD, PhD    31715264400    M.Roestenberg@lumc.nl    Principal Investigator: Leo G. Visser, MD          Radboud University Medical Center, Geert Grooteplein 28 Recruiting Nijmegen, Netherlands, 6525 GA Contact: Robert W. Sauerwein, MD    31243610577    Robert.Sauerwein@radboudumc.nl    Contact: Jona Walk, MD    31243613663    Jona.Walk@radboudumc.nl    Principal Investigator: Robert W. Sauerwein, MD 收起 <<
NCT01218893 Plasmodium Falciparum Malaria Not Applicable Completed - Netherlands ... 展开 >> Leiden University Medical Centre Leiden, Netherlands, 2300 RC 收起 <<
NCT01236612 Plasmodium Falciparum Malaria Not Applicable Completed - Netherlands ... 展开 >> Radboud University Nijmegen Medical Centre Nijmegen, Netherlands, 6500 HB 收起 <<

Atovaquone/阿托伐醌 参考文献

[1]Kessl JJ, Lange BB, et al. Molecular basis for atovaquone binding to the cytochrome bc1 complex. J Biol Chem. 2003 Aug 15;278(33):31312-8.

[2]Looareesuwan S, Viravan C, et al. Clinical studies of atovaquone, alone or in combination with other antimalarial drugs, for treatment of acute uncomplicated malaria in Thailand. Am J Trop Med Hyg. 1996 Jan;54(1):62-6.

[3]Azami SJ, Amani A, Keshavarz H, et al. Nanoemulsion of atovaquone as a promising approach for treatment of acute and chronic toxoplasmosis. Eur J Pharm Sci. 2018;117:138‐146

[4]Schöler N, Krause K, Kayser O, et al. Atovaquone nanosuspensions show excellent therapeutic effect in a new murine model of reactivated toxoplasmosis. Antimicrob Agents Chemother. 2001;45(6):1771‐1779

[5]Patel M, Johnson M, Sychterz CJ, et al. Hepatobiliary Disposition of Atovaquone: A Case of Mechanistically Unusual Biliary Clearance. J Pharmacol Exp Ther. 2018;366(1):37‐45

[6]Fiorillo M, Lamb R, Tanowitz HB, et al. Repurposing atovaquone: targeting mitochondrial complex III and OXPHOS to eradicate cancer stem cells. Oncotarget. 2016;7(23):34084‐34099

Atovaquone/阿托伐醌 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.63mL

2.73mL

1.36mL

27.26mL

5.45mL

2.73mL

Atovaquone/阿托伐醌 技术信息

CAS号95233-18-4
分子式C22H19ClO3
分子量 366.84
SMILES Code O=C1C([C@H]2CC[C@H](C3=CC=C(Cl)C=C3)CC2)=C(O)C(C4=C1C=CC=C4)=O
MDL No. MFCD00889188
别名 Atavaquone; BW 566C; Wellvone; Mepron; hydroxynaphthoquinone 566C80; GlaxoSmithKline brand of atovaquone; Glaxo Wellcome brand of atovaquone; compound 566; atovaquone GlaxoSmithKline brand; 566C80 hydroxynaphthoquinone; 566C80; 566C; BW 556C-80
运输蓝冰
InChI Key BSJMWHQBCZFXBR-UHFFFAOYSA-N
Pubchem ID 74989
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C
动物实验配方

5% DMSO+corn oil 0.5 mg/mL

Tags: Atovaquone | 95233-18-4 | Atavaquone | Parasite | Anti-infection | Metabolic Enzyme/Protease | Parasite | Cytochrome P450 | Antibiotic | Bacterial | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Atovaquone/阿托伐醌 纯度/质量文件 | Atovaquone/阿托伐醌 生物活性 | Atovaquone/阿托伐醌 临床数据 | Atovaquone/阿托伐醌 参考文献 | Atovaquone/阿托伐醌 实验方案 | Atovaquone/阿托伐醌 技术信息

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