Valinomycin
(Synonyms: 缬氨霉素,NSC 122023) 目录号 : GC16948缬霉素Valinomycin是一种十二肽抗生素,从几种链霉菌菌株中获得。
Cas No.:2001-95-8
Sample solution is provided at 25 µL, 10mM.
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Valinomycin is a dodecadepsipeptide antibiotic, which is obtained from several Streptomyces strains. Valinomycin functions as a potassium-specific transporter and promotes the movement of K+ through lipid membranes. Excessive K+ efflux is an ionic mechanism underlying apoptosis.It can be used as uncoupling agent to induce depolarization[1-3].
Valinomycin(1-100µM;12-24 h) treated CHO cells underwent an apoptotic event due to potassium efflux[4]. Valinomycin (2 nM) induced energy-dependent mitochondrial swelling, cytochrome c release, cytosolic NADH/cytochrome c oxidation and apoptosis[5]. Neurite formation and membrane changes of mouse neuroblastoma cells induced by valinomycin(100 µM) [6].
Incorporation of valinomycin into multilamellar liposomes composed of dimyristoyl phosphatidyl choline:cholesterol:phosphatidyl serine (10:4:1 M ratio) results in a profound reduction in toxicity with maintainence of antitumor efficacy in mice, the LD50 for liposome incorporated valinomycin (MVL-VM) is in excess of 50 mg/kg[7].
References:
[1]. Varma S, Sabo D, ,et,al. K+/Na+ selectivity in K channels and valinomycin: over-coordination versus cavity-size constraints. J Mol Biol. 2008 Feb 8;376(1):13-22. doi: 10.1016/j.jmb.2007.11.059. Epub 2007 Nov 28. PMID: 18155244; PMCID: PMC2390915.
[2]. Daniele RP, Holian SK. A potassium ionophore (valinomycin) inhibits lymphocyte proliferation by its effects on the cell membrane. Proc Natl Acad Sci U S A. 1976 Oct;73(10):3599-602. doi: 10.1073/pnas.73.10.3599. PMID: 1068473; PMCID: PMC431165.
[3]. Berezin SK. Valinomycin as a Classical Anionophore: Mechanism and Ion Selectivity. J Membr Biol. 2015 Aug;248(4):713-26. doi: 10.1007/s00232-015-9784-y. Epub 2015 Mar 4. PMID: 25736817.
[4]. Abdalah R, Wei L, ,et,al. Valinomycin-induced apoptosis in Chinese hamster ovary cells. Neurosci Lett. 2006 Sep 11;405(1-2):68-73. doi: 10.1016/j.neulet.2006.06.055. Epub 2006 Jul 20. PMID: 16857314.
[5]. Lofrumento DD, La Piana G, ,et,al. Valinomycin induced energy-dependent mitochondrial swelling, cytochrome c release, cytosolic NADH/cytochrome c oxidation and apoptosis. Apoptosis. 2011 Oct;16(10):1004-13. doi: 10.1007/s10495-011-0628-7. PMID: 21739274.
[6]. Koike T. Neurite formation and membrane changes of mouse neurobalstoma cells induced by valinomycin. Biochim Biophys Acta. 1978 Jun 2;509(3):429-39. doi: 10.1016/0005-2736(78)90237-7. PMID: 656419.
[7]. Daoud SS, Juliano RL. Reduced toxicity and enhanced antitumor effects in mice of the ionophoric drug valinomycin when incorporated in liposomes. Cancer Res. 1986 Nov;46(11):5518-23. PMID: 3756900.
缬霉素Valinomycin是一种十二肽抗生素,从几种链霉菌菌株中获得。Valinomycin作为钾特异性转运体,促进钾离子通过脂质膜的运动。过量的K+外排是细胞凋亡的离子机制。它可以作为解偶联剂来诱导去极化[1-3]。
Valinomycin (1-100µM;12-24 h)处理的CHO细胞由于钾外排而发生凋亡事件[4]。Valinomycin (2 nM)诱导能量依赖性线粒体肿胀、细胞色素C释放、胞浆NADH/细胞色素c氧化和细胞凋亡[5]。Valinomycin (100 µM)诱导小鼠神经母细胞瘤细胞的神经突形成和膜的改变[6]。
将Valinomycin掺入由二肉豆醇磷脂酰胆碱:胆固醇:磷脂酰丝氨酸(10:4:1)组成的多层脂质体中,可显著降低小鼠的毒性并保持抗肿瘤功效,掺入缬霉素脂质体的LD50超过50 mg/kg[7]。
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Cell experiment [1]: |
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Cell lines |
CHO cells |
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Preparation method |
Valinomycin is added into the culture medium. |
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Reaction Conditions |
1-100μM;12-24 h |
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Applications |
100 μM valinomycin caused 77% and 86% cell death at 12 h and 24 h, respectively. |
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References: [1]. Abdalah R, Wei L,et,al. Valinomycin-induced apoptosis in Chinese hamster ovary cells. Neurosci Lett. 2006 Sep 11;405(1-2):68-73. doi: 10.1016/j.neulet.2006.06.055. Epub 2006 Jul 20. PMID: 16857314. |
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| Cas No. | 2001-95-8 | SDF | |
| 别名 | 缬氨霉素,NSC 122023 | ||
| 化学名 | (3S,6R,9R,12S,15S,18S,21R,24R,27R,30R,33R,36S)-3,6,9,15,18,21,27,30,33-nonaisopropyl-12,24,36-trimethyl-1,7,13,19,25,31-hexaoxa-4,10,16,22,28,34-hexaazacyclohexatriacontane-2,5,8,11,14,17,20,23,26,29,32,35-dodecaone | ||
| Canonical SMILES | O=C([C@@H](C(C)C)OC([C@@H](C(C)C)NC1=O)=O)N[C@@H](C(O[C@H](C)C(N[C@@H](C(O[C@H](C(N[C@H](C(O[C@@H](C)C(N[C@@H](C(O[C@@H](C(N[C@H](C(O[C@H]1C)=O)C(C)C)=O)C(C)C)=O)C(C)C)=O)=O)C(C)C)=O)C(C)C)=O)C(C)C)=O)=O)C(C)C | ||
| 分子式 | C54H90N6O18 | 分子量 | 1111.32 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 5 mg/ml,Ethanol: 10 mg/ml | 储存条件 | Store at -20°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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.8998 mL | 4.4992 mL | 8.9983 mL |
| 5 mM | 0.18 mL | 0.8998 mL | 1.7997 mL |
| 10 mM | 0.09 mL | 0.4499 mL | 0.8998 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet