Verruculogen
(Synonyms: 疣孢青霉原) 目录号 : GC17001A tremorgenic mycotoxin
Cas No.:12771-72-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Verruculogen is a Maxi-K potassium channels inhibitor.
Maxi-K, a potassium channel characterized by their large conductance for potassium ions through cell membranes, is activated by changes in membrane electrical potential and/or by increases in concentration of intracellular calcium ion. Maxi-K channels are critical for the regulation of several key physiological processes, such as smooth muscle tone and neuronal excitability.
In vitro: In a previous study, it was found that aflatrem, paspalitrem A, paspalitrem C, penitrem A, and paspalinine could inhibit the binding of [125I]charybdotoxin to maxi-K channels in bovine aortic smooth muscle sarcolemmal membranes. Whereas, verruculogen enhanced toxin binding. Despite their different effects on binding of [125I]charybdotoxin to maxi-K channels, all tested compounds including verruculogen were able to potently inhibit maxi-K channels in electrophysiological experiments, and other types of voltage-dependent or Ca(2+)-activated K+ channels examined were not affected [1].
In vivo: In an animal study, the mechanism of the genesis of tremor induced by verruculogen was investigated. It was found that atropine, glycine, mephenesin, and penicillamine with proven efficacy in relieving tremor of varied etiology, failed to modify verruculogen induced tremor. Oxyaminoacetic acid, which raises the CNS levels of GABA, and beta (chlorphenyl) gamma aminobutyric acid, which passes the hematoencephalic barrier, completely or partly relieved tremor and other verruculogen-induced symptoms, depending on the dose of the verruculogen administered. Picrotoxin, a GABA antagonist, increased the effect of verruculogen in the tested animals [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Knaus, H. G.,McManus, O.B.,Lee, S.H., et al. Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33(19), 5819-5828 (1994).
[2] Hotujac L, Stern P. Pharmacological examination of verruculogen induced tremor. Acta Med Iugosl. 1974;28(3):223-9.
Cas No. | 12771-72-1 | SDF | |
别名 | 疣孢青霉原 | ||
化学名 | (5R,10S,10aR)-1,10,10a,14,14aS,15bS-hexahydro-10,10a-dihydroxy-7-methoxy-2,2-dimethyl-5-(2-methyl-1-propen-1-yl)-5H,12H-3,4-dioxa-5a,11a,15a-triazacyclooct[lm]indeno[5,6-b]fluorene-11,15(2H,13H)-dione | ||
Canonical SMILES | O=C1N2[C@](CCC2)([H])C(N3[C@@H]4C5=C(C(C=CC(OC)=C6)=C6N5[C@@H](/C=C(C)/C)OOC(C)(C)C4)[C@H](O)[C@]31O)=O | ||
分子式 | C27H33N3O7 | 分子量 | 511.6 |
溶解度 | Soluble in ethanol;Soluble in methanol;Soluble in DMSO;Soluble in dimethyl formamide | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.9547 mL | 9.7733 mL | 19.5465 mL |
5 mM | 0.3909 mL | 1.9547 mL | 3.9093 mL |
10 mM | 0.1955 mL | 0.9773 mL | 1.9547 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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