Atovaquone
(Synonyms: 阿托伐醌; Atavaquone) 目录号 : GC17903
An antiprotozoal agent
Cas No.:95233-18-4
Sample solution is provided at 25 µL, 10mM.
Atovaquone is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.Target: AntiparasiticAtovaquone (atavaquone) is a chemical compound that belongs to the class of naphthalenes. Atovaquone is a hydroxy-1,4-naphthoquinone, an analog of ubiquinone, with antipneumocystic activity [1]. Atovaquone is an anti-protozoal mitochondrial electron transport inhibitor; Antimalarial; Antipneumocystic, and has also been used to treat toxoplasmosis. It acts by inhibiting the cytochrome bc(1) complex via interactions with the Rieske iron-sulfur protein and cytochrome b in the ubiquinol oxidation pocket [2]. Atovaquone is a unique naphthoquinone with broad-spectrum antiprotozoal activity. It is effective for the treatment and prevention of Pneumocystis carinii pneumonia (PCP), it is effective in combination with proguanil for the treatment and prevention of malaria, and it is effective in combination with azithromycin for the treatment of babesiosis [3].
References:
[1]. Looareesuwan, S., 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. 54(1): p. 62-6.
[2]. Kessl, J.J., et al., Molecular basis for atovaquone binding to the cytochrome bc1 complex. J Biol Chem, 2003. 278(33): p. 31312-8.
[3]. Baggish, A.L. and D.R. Hill, Antiparasitic agent atovaquone. Antimicrobial agents and chemotherapy, 2002. 46(5): p. 1163-1173.
| In vitro experiment [1]: | |
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Parasites |
B. gibsoni |
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Preparation method |
The solubility of this compound in DMSO is >17.03mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 3.2 μM |
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Applications |
The ΣFICs against WT B. gibsoni were 0.93, 0.82, 0.83 and 0.96 for Atovaquone and Proguanil at a ratio of 4:1, 3:2, 2:3 and 1:4, respectively. The ΣFICs against Atovaquone-resistant B. gibsoni were 0.88, 0.60, 0.77 and 0.88 at each ratio. The results implied that Atovaquone synergized the effects of Proguanil on WT and Atovaquone-resistant B. gibsoni. |
| Animal experiment [1]: | |
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Animal models |
Dogs infected with B. gibsoni |
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Dosage form |
17 ~ 25 mg/kg; p.o. |
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Applications |
In B. gibsoni-infected dogs, the combination of Atovaquone and Proguanil alleviated parasitemia. However, all dogs showed relapse of parasitic infection. In addition, some side effects were also observed. Self-limiting vomiting occurred in 2 dogs and hyperphosphatasia occurred in another dog. Mild increases in the alanine aminotransferase levels were confirmed in 2 dogs. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Iguchi A, Matsuu A, Fujii Y, Ikadai H, Hikasa Y. The in vitro interactions and in vivo efficacy of atovaquone and proguanil against Babesia gibsoni infection in dogs. Vet Parasitol. 2013 Nov 8;197(3-4):527-33. | |
| Cas No. | 95233-18-4 | SDF | |
| 别名 | 阿托伐醌; Atavaquone | ||
| 化学名 | 3-(4-(4-chlorophenyl)cyclohexyl)-4-hydroxynaphthalene-1,2-dione | ||
| Canonical SMILES | ClC1=C([H])C([H])=C(C([H])=C1[H])C2([H])C([H])([H])C([H])([H])C(C(C3=O)=C(C4=C([H])C([H])=C([H])C([H])=C4C3=O)O[H])([H])C([H])([H])C2([H])[H] | ||
| 分子式 | C22H19ClO3 | 分子量 | 366.84 |
| 溶解度 | ≥ 17.03mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.726 mL | 13.6299 mL | 27.2598 mL |
| 5 mM | 0.5452 mL | 2.726 mL | 5.452 mL |
| 10 mM | 0.2726 mL | 1.363 mL | 2.726 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet