Tetrodotoxin citrate

Name: Tetrodotoxin citrate
Brand: Tocris Bioscience
SKU: 1069
Rating: 4 (3 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1069

(3)

Citations (487)

COA / SDS

Na+ channel blocker; citrate salt of tetrodotoxin (Cat. No. 1078)

Key Product Details

Description:	Na⁺ channel blocker; citrate salt of tetrodotoxin (Cat. No. 1078)
Alternative Names:	TTx citrate
Chemical Name:	(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 citrate
Purity:	≥98% (HPLC)
Molecular Weight:	319.27

View Full Technical Details for Tetrodotoxin citrate

Technical Data
Citations / Reviews (3)

Biological Activity for Tetrodotoxin citrate

Tetrodotoxin citrate, the water-soluble citrate salt of tetrodotoxin, is a reversible, potent, selective and high affinity inhibitor of voltage gated sodium channels Na_v 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 (K_d = 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⁺ (Ca_v1.x) channels, blocks primary reward in an animal study of drug-seeking lever pressing.

Tetrodotoxin (Cat. No. 1078) also available.

Technical Data for Tetrodotoxin citrate

M. Wt	319.27
Formula	C₁₁H₁₇N₃O₈
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	18660-81-6
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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Tetrodotoxin citrate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	31.93	100

Preparing Stock Solutions for Tetrodotoxin citrate

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.13 mL	15.66 mL	31.32 mL
5 mM	0.63 mL	3.13 mL	6.26 mL
10 mM	0.31 mL	1.57 mL	3.13 mL
50 mM	0.06 mL	0.31 mL	0.63 mL

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References for Tetrodotoxin citrate

References are publications that support the biological activity of the product.

Shoromony Prolonged duration local anesthesia by combined delivery of capsaicin- and tetrodotoxin-loaded liposomes. Anesth.Analg. 2019 PMID: 31425210
Ono Antagonistic effects of tetrodotoxin on aconitine-induced cardiac toxicity. J.Nippon Med.Sch. 2013 PMID: 24189353
Tsukamoto Differential binding of tetrodotoxin and its derivatives to voltage-sensitive sodium channel subtypes (Nav1.1 to Nav1.7). Br.J.Pharmacol. 2017 PMID: 28832970
Hegyi Tetrodotoxin blockade on canine cardiac L-type Ca²⁺ channels depends on pH and redox potential. Mar.Drugs 2013 PMID: 23771047
Grimm and See Dissociation of primary and secondary reward-relevant limbic nuclei in an animal model of relapse. Neuropsychopharmacology 2000 PMID: 10731622
Kao Structure-activity relations of tetrodotoxin, saxitoxin, and analogues. Ann.N.Y.Acad.Sci. 1986 PMID: 2434008
Kao Pharmacology of tetrodotoxin and saxitoxin. Fed.Proc. 1972 PMID: 5032475
Gleitz The protective action of tetrodotoxin and (±)-kavain on anaerobic glycolysis, ATP content and intracellular Na⁺ and Ca²⁺ of anoxic brain vesicles. Neuropharmacology 1996 PMID: 9076753