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Submit ReviewTetrodotoxin
说明： Na+ channel blocker
别名： TTx
化学名： (4R,4aR,5R,7S,9S,10S,10aR,11S,12S)-Octahydro-12-(hydroxymethyl)-2-imino-5,9:7,10a-dimethano-10aH-[1,3]dioxocino[6,5-d]pyrimidine-4,7,10,11,12-pentol
纯度： ≥98% (HPLC)
生物活性 for Tetrodotoxin
Tetrodotoxin is a reversible, potent, selective and high affinity inhibitor of voltage gated sodium channels Nav 1.6, 1.1, 1.3, 1.4, 1.2 and 1.7 (IC50 values are 2.3 nM, 4.1 nM, 5.3 nM, 7.6 nM, 14 nM and 36 nM, respectively). Binding is reversible and high affinity (Kd = 1-10 nM). Tetrodotoxin shows antagonism of aconitine-induced cardiac toxicity, analgesic effects in mouse models of neuropathy and prolonged duration of local anesthesia in animals when combined with capsaicin. Tetrodotoxin also shows pH-dependent blockade of canine cardiac L-type Ca2+ (Cav1.x) channels, blocks primary reward in an animal study of drug-seeking lever pressing.
Tetrodotoxin citrate (Cat. No. 1069) also available.
技术数据 for Tetrodotoxin
| 分子量 | 319.27 |
| 公式 | C11H17N3O8 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 4368-28-9 |
| PubChem ID | 16759596 |
| InChI Key | CFMYXEVWODSLAX-CKYAAQHSSA-N |
| Smiles | OC1(CO)[C@H](O4)C(O)[C@@]2([C@@H]([C@@H](O)N3)C1O[C@](O)4[C@H]2O)NC3=N |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Tetrodotoxin
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| acidic buffer (pH 4.8) | 0.96 | 3 |
制备储备液 for Tetrodotoxin
以下数据基于产品分子量 319.27。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.03 mM | 104.4 mL | 522.02 mL | 1044.05 mL |
| 0.15 mM | 20.88 mL | 104.4 mL | 208.81 mL |
| 0.3 mM | 10.44 mL | 52.2 mL | 104.4 mL |
| 1.5 mM | 2.09 mL | 10.44 mL | 20.88 mL |
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产品说明书 for Tetrodotoxin
参考文献 for Tetrodotoxin
参考文献是支持产品生物活性的出版物。
Gleitz et al (1996) The protective action of tetrodotoxin and (±)-kavain on anaerobic glycolysis, ATP content and intracellular Na+ and Ca2+ of anoxic brain vesicles. Neuropharmacology 35 1743 PMID: 9076753
Kao (1972) Pharmacology of tetrodotoxin and saxitoxin. Fed.Proc. 31 1117 PMID: 5032475
Kao (1986) Structure-activity relations of tetrodotoxin, saxitoxin, and analogues. Ann.N.Y.Acad.Sci. 479 52 PMID: 2434008
Merck Index 12 9382
Tsukamoto et al (2017) Differential binding of tetrodotoxin and its derivatives to voltage-sensitive sodium channel subtypes (Nav1.1 to Nav1.7). Br.J.Pharmacol. 174 3881 PMID: 28832970
Ono et al (2013) Antagonistic effects of tetrodotoxin on aconitine-induced cardiac toxicity. J.Nippon Med.Sch. 80 350 PMID: 24189353
Hegyi et al (2013) Tetrodotoxin blockade on canine cardiac L-type Ca²+ channels depends on pH and redox potential. Mar.Drugs 11 2140 PMID: 23771047
Grimm and See (2000) Dissociation of primary and secondary reward-relevant limbic nuclei in an animal model of relapse. Neuropsychopharmacology 22 473 PMID: 10731622
Shomorony et al (2019) Prolonged duration local anesthesia by combined delivery of capsaicin- and tetrodotoxin-loaded liposomes. Anesth.Analg. 129 709 PMID: 31425210
If you know of a relevant reference for Tetrodotoxin, please let us know.
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关键词: Tetrodotoxin, Tetrodotoxin supplier, Na+, channel, blockers, Sodium, NaV, Channels, voltage-gated, voltage-dependent, TTx, Voltage-gated, 1078, Tocris Bioscience
337 篇 Tetrodotoxin 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Tetrodotoxin 的部分引用包括：
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Tetrodotoxin 的评论
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Totally blocked action potential.
By
Yuyang Sun on 05/30/2022
分析类型： In Vitro
种属： Mouse
Works great. Totally blocked the action potential in mouse brain slice.
Validation.
By
Anonymous on 04/04/2020
分析类型： In Vitro
种属： Rat
细胞系/组织： Sprague-Dawley rats primary neuronal
10 μM for 30min
The pharmacological inhibitors for electrophysiology assay.
By
Anonymous on 02/28/2020
分析类型： In Vitro
种属： Other
The following concentrations we were used:1 μM Bay K, 10 μM nifedipine, 10 μM nimodipine, 300 nM omega -agatoxin, 1 μM omega -conotoxin, 5 μM mibefradil, 1 μM tetrodotoxin, 1 μM charybdotoxin, 100 nM iberiotoxin, 10 μM NS11021.
TTX blocks action potential propagation.
By
Anonymous on 08/31/2019
分析类型： Ex Vivo
种属： Rat
细胞系/组织： Hippocampus
Tetrodotoxin (TTX) was used to block action potential propagation in response to lasting current injection into living neuron. This illustrated a critical role of voltage-gated sodium channels in inter-neuronal crosstalk. 1 microM of TTX developed 100% effect (see Figure). Figure: action potential generation by isolated neuron under control and after TTX was added to perfusion solution.
Compound should be sonicated when dissolved.
good drug for neuronal activity inhibition.
By
Lihua Wang on 01/24/2018
分析类型： In Vitro
种属： Mouse
We use this to block cell activity of the brain slices, in order to keep the cells more healthy after they are dissociated. It works great and helps a lot for our purpose; but the only little problem is that it's very hard to dissolve in the water.