Atractyloside Dipotassium Salt
(Synonyms: 苍术苷钾盐) 目录号 : GC15878
Inhibitor of ADP/ATP translocases
Cas No.:102130-43-8
Sample solution is provided at 25 µL, 10mM.
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Atractyloside Dipotassium Salt is an inhibitor of ADP/ATP Translocase.
ATP-ADP translocase (AAT) is a mitochondrial ADP/ATP carrier. It transports ATP from the mitochondrial matrix to the cytoplasm and transports ADP from the cytoplasm to the mitochondrial matrix.
In Ehrlich ascites tumor cells, atractyloside (3 mM) inhibited cells growth by 70%. The mitochondria became spherical shaped with translucent matrix rid of cristae. When transfered to normal medium, proliferation and macromolecular synthesis recovered to normal levels within 3 to 6 h [2].
In the sarcoplasmic reticulum vesicles from the rabbit skeletal muscle with 10 μM of cytoplasmic Ca2+, atractyloside reduced the rate of choline+ influx through the Ca2+ channels to 60%. Also, it inhibited about half of Ca2+ channels incorporated into planar bilayers [1]. In mitochondrial membranes isolated from a rat heart muscle, atractyloside (5-100 μM) inhibited the chloride channels in dose-dependent way [3].
References:
[1]. Yamaguchi N, Kagari T, Kasai M. Inhibition of the ryanodine receptor calcium channel in the sarcoplasmic reticulum of skeletal muscle by an ADP/ATP translocase inhibitor, atractyloside. Biochem Biophys Res Commun, 1999, 258(2): 247-251.
[2]. Pick-Kober KH, Schneider F. Proliferation, macromolecular synthesis and energy metabolism of in vitro grown Ehrlich ascites tumor cells after inhibition of ATP-ADP translocation by atractyloside. Eur J Cell Biol, 1984, 34(2): 323-329.
[3]. Malekova L, Kominkova V, Ferko M, et al. Bongkrekic acid and atractyloside inhibits chloride channels from mitochondrial membranes of rat heart. Biochim Biophys Acta, 2007, 1767(1): 31-44.
| Cell experiment [1-3]: | |
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Cell lines |
Ehrlich ascites tumor cells, J2-3T3 cells and cervical carcinoma cells |
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Preparation method |
The solubility of this compound in DMSO is > 37.05 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
3 mM, 24 h |
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Applications |
In cultured Ehrlich ascites tumor cells, atractyloside (3 mM, 24 h) inhibited cell growth by 70% with not severe influence on cell viability. Atractyloside retarded cell cycle progression. After transfer of atractyloside treated cells to normal medium, proliferation and macromolecular synthesis normalized within 3 to 6 h. Atractyloside increased glucose consumption and lactate production. Lactate/glucose ratio was 1.9 after 24 h. Atractyloside reduced oxygen uptake. Atractyloside increased the ATP/ADP concentration ratio in the mitochondrial and extramitochondrial compartment. Atractyloside dose-dependently induced apoptosis in normal J2-3T3 cells and cervical carcinoma cells by loss of cell viability, nuclear fragmentation and DNA laddering. The sensitivity of cells to atractyloside-induced apoptosis was found to be: HPV 16 E6-J2-3T3 > CaSki > normal-J2-3T3 cells approximately ts p53-J2-3T3 approximately vector-J2-3T3 cells > Hela > SiHa > C33A approximately C33A 16 E6. Atractyloside can induce opening of the mitochondrial permeability transition pore (mPTP) in arteriolar smooth muscle cells (ASMCs). Treatment with 7.5, 10, and 15 μM atractyloside for 10 min significantly reduced the relative ATP content in ASMCs by 48%, 63% and 66% of control, and ASMCs were hyperpolarized. |
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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]. Pick-Kober K H, Schneider F. Proliferation, macromolecular synthesis and energy metabolism of in vitro grown Ehrlich ascites tumor cells after inhibition of ATP-ADP translocation by atractyloside[J]. European journal of cell biology, 1984, 34(2): 323-329. [2]. Brown J, Higo H, Mckalip A, et al. Human papillomavirus (HPV) 16 E6 sensitizes cells to atractyloside‐induced apoptosis: Role of p53, ICE‐like proteases and the mitochondrial permeability transition[J]. Journal of cellular biochemistry, 1997, 66(2): 245-255. [3]. Song R, Bian H, Huang X, et al. Atractyloside induces low contractile reaction of arteriolar smooth muscle through mitochondrial damage[J]. Journal of Applied Toxicology, 2012, 32(6): 402-408. | |
| Cas No. | 102130-43-8 | SDF | |
| 别名 | 苍术苷钾盐 | ||
| 化学名 | potassium (2R,3R,4R,5R,6S)-6-(((2aR,3R,5R,6aR,6bS,9R,11S,11aR)-3-carboxy-11-hydroxy-6a-methyl-10-methylenetetradecahydro-9,11a-methanocyclohepta[a]naphthalen-5-yl)oxy)-2-(hydroxymethyl)-5-((3-methylbutanoyl)oxy)tetrahydro-2H-pyran-3,4-diyl bis(sulfate) | ||
| Canonical SMILES | CC(C)CC(=O)OC1C(C(C(OC1OC2CC(C3CCC45CC(CCC4C3(C2)C)C(=C)C5O)C(=O)O)CO)OS(=O)(=O)[O-])OS(=O)(=O)[O-].[K+].[K+] | ||
| 分子式 | C30H44K2O16S2 | 分子量 | 802.99 |
| 溶解度 | ≥ 37.05mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2453 mL | 6.2267 mL | 12.4535 mL |
| 5 mM | 0.2491 mL | 1.2453 mL | 2.4907 mL |
| 10 mM | 0.1245 mL | 0.6227 mL | 1.2453 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