ω-Conotoxin GVIA
(Synonyms: Ω-芋螺毒素) 目录号 : GC13886
ω-芋螺毒素 GVIA （ω-Conotoxin GVIA）是一种锥形蜗牛毒素，可选择性地阻断神经元中的 N 型通道。
Cas No.:106375-28-4
Sample solution is provided at 25 µL, 10mM.
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ω-Conotoxin GVIA is a cone snail toxin that selectively blocks N-type channels in neurons [1].
ω-Conotoxin GVIA binds to human neocortical, rat hippocampal, and chick brain synaptic plasma membranes (IC50s = 4.6, 60, and 150 pM, respectively, in radioligand binding assays) [3,4,5].
ω-Conotoxin GVIA markedly reduced the amplitude of the tetanic contractions of the tibialis anterior muscle in mice, but tetanic facilitation was not impaired. The muscle contractions elicited by direct electrical stimulation were not significantly modified by ω-Conotoxin GVIA. ω-Conotoxin GVIA did not had any significant changes in systemic blood pressure [5].
References:
[1]. H.D. Mansvelder, J.C. Stoof, K.S. Kits. Dihydropyridine block of ω-agatoxin IVA- and ω-conotoxin GVIA-sensitive Ca2+ channels in rat pituitary melanotropic cells.Eur. J. Pharmacol., 311 (1996), pp. 293-304
[2]. Feuerstein, T.J., Dooley, D.J., and Seeger, W. Inhibition of norepinephrine and acetylcholine release from human neocortex by ω-conotoxin GVIA. J. Pharmacol. Exp. Ther. 252(2), 778-785 (1990).
[3]. Lampe, R.A., Lo, M.M., Keith, R.A., et al. Effects of site-specific acetylation on ω-conotoxin GVIA binding and function. Biochemistry 32(13), 3255-3260 (1993).
[4]. Sato, K., Park, N.G., Kohno, T., et al. Role of basic residues for the binding of ω-conotoxin GVIA to N-type calcium channels. Biochem. Biophys. Res. Commun. 194(3), 1292-1296 (1993).
[5]: Rossoni G, Berti F, La Maestra L, Clementi F. ω-Conotoxin GVIA binds to and blocks rat neuromuscular junction. Neuroscience Letters. 1994;176:185-188.
ω-芋螺毒素 GVIA （ω-Conotoxin GVIA）是一种锥形蜗牛毒素，可选择性地阻断神经元中的 N 型通道[1]。
ω-芋螺毒素 GVIA 与人类新皮质、大鼠海马和鸡脑突触质膜结合（在放射性配体结合试验中,IC50 分别 = 4.6、60 和 150 pM）[3,4,5].
ω-芋螺毒素 GVIA 显着降低了小鼠胫骨前肌的强直收缩幅度,但强直易化作用并未受损。 ω-芋螺毒素 GVIA 未显着改变由直接电刺激引起的肌肉收缩。 ω-芋螺毒素 GVIA 对体循环血压无明显影响[5]。
| Cell experiment [1]: | |
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Cell lines |
Rat pituitary melanotropic cells |
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Preparation Method |
ω-Conotoxin GVIA was administered via a gravity-driven Y-tube system or pressure jet. The recording chamber was continuously perfused at a rate of ~ 1.5ml/min, driven by air pressure, and the bath volume was kept constant by continuous suction. Electrophysiological testing was performed. |
|
Reaction Conditions |
1 or 10 µM |
|
Applications |
1 µM ω-Conotoxin GVIA blocked the high voltage-activated current by 25.5±3.6%. The block at 10µM ω-Conotoxin GVIA was 22.9±2.5% (not significantly different from the block by 1µM;n = 3), indicating thatω-Conotoxin GVIA yields a saturating effect. |
| Animal experiment [2]: | |
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Animal models |
male COBS CD (SD) rats |
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Preparation Method |
After intravenous injection of different doses of ω-Conotoxin GVIA (1--2 nmol/kg) in rats, the sciatic nerve of the rats was stimulated and the blood pressure of the rats was measured through the carotid artery. |
|
Dosage form |
Intravenous injection, 1--2 nmol/kg |
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Applications |
IIntravenous injection caused a progressive loss of tension development of tibialis muscle indirectly evoked by the electrical stimulation of the sciatic nerve, ω-Conotoxin GVIA (1 nmol/kg i.v.) reduced the strength of muscle contraction by 75% in about 27 min (from 39.5 + 1.8 g to 9.9 + 0.4 g). |
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References: [1]: H.D. Mansvelder, J.C. Stoof, K.S. Kits. Dihydropyridine block of ω-agatoxin IVA- and ω-conotoxin GVIA-sensitive Ca2+ channels in rat pituitary melanotropic cells.Eur. J. Pharmacol., 311 (1996), pp. 293-304 |
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| Cas No. | 106375-28-4 | SDF | |
| 别名 | Ω-芋螺毒素 | ||
| Canonical SMILES | C[C@](O)([H])[C@@](/N=C(O)/[C@](/N=C(O)/[C@]1([H])C[C@](O)([H])CN12)([H])CC3=CC=C(O)C=C3)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N\[C@@](/C(O)=N\[C@@](C(O)=N)([H])CC4=CC=C(O)C=C4)([H])CSSC[C@@](N=C(O)[C@](N=C(O)[C@](N=C(O)[C@](N=C(O)[C@](N=C(O)[C@]5([H])C[ | ||
| 分子式 | C120H182N38O43S6 | 分子量 | 3037.35 |
| 溶解度 | Soluble to 1 mg/ml in Water | 储存条件 | Desiccate 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.3292 mL | 1.6462 mL | 3.2923 mL |
| 5 mM | 0.0658 mL | 0.3292 mL | 0.6585 mL |
| 10 mM | 0.0329 mL | 0.1646 mL | 0.3292 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