| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Ki: 1.25 nM ( α4β2 receptor) Ki: 1.84 μM ( α7 receptor)[1]
(±)-Anatoxin A fumarate targets nicotinic acetylcholine receptors (nAChRs). It is a potent nicotinic agonist with high affinity, showing Ki values of 1.25 nM for the α4β2 receptor and 1840 nM for the α7 receptor. Its strong agonist activity at these receptors underlies its neurotoxic effects and its use as a research tool. |
|---|---|
| ln Vitro |
In vitro, (±)-Anatoxin A fumarate is a potent nicotinic agonist with Ki values of 1.25 nM for α4β2 and 1840 nM for α7 nAChRs. It stimulates [3H]-dopamine release from rat striatal synaptosomes with an EC50 of 134 nM. These activities confirm its high potency and mechanism of action as a nAChR agonist.
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| ln Vivo |
In vivo, (±)-Anatoxin A fumarate is a potent cyanotoxin with acute neurotoxicity. It can cause loss of coordination, muscular fasciculations, convulsions, and death by respiratory paralysis. Its potent neurotoxic effects are used in research to model excitotoxicity and to study the mechanisms of cholinergic overstimulation.
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| Enzyme Assay |
Non-cell-based assays for (±)-Anatoxin A fumarate typically involve radioligand binding studies to determine its affinity (Ki) for nAChR subtypes. Membrane preparations from cells or tissues expressing specific nAChRs are incubated with a radiolabeled ligand and varying concentrations of the compound. The Ki values (e.g., 1.25 nM for α4β2, 1840 nM for α7) are calculated from displacement curves.
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| Cell Assay |
For in vitro cellular assays, synaptosomal preparations or neuronal cell lines are used. The compound's ability to stimulate neurotransmitter release, such as [3H]-dopamine from striatal synaptosomes (EC50 = 134 nM), is a key functional readout. This confirms its agonist activity and allows for the study of its signaling pathways.
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| Animal Protocol |
In vivo animal studies with (±)-Anatoxin A fumarate involve administering the compound to rodents, often via intravenous or intracerebroventricular injection. The resulting neurotoxic effects, such as muscle fasciculations, convulsions, and respiratory paralysis, are observed. This model is used to study excitotoxicity and to test potential therapeutic countermeasures.
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| ADME/Pharmacokinetics |
(±)-Anatoxin A fumarate has a molecular weight of 281.30 g/mol. Its CAS number is 1219922-30-1. It is a racemic mixture of the naturally occurring toxin. It is a potent research chemical and should be handled with extreme caution due to its high toxicity. It is for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of (±)-Anatoxin A fumarate is defined by its potent neurotoxicity. It causes acute poisoning by overstimulating nicotinic receptors, leading to respiratory paralysis. Due to its extreme toxicity, it is a hazardous substance and must be handled only by trained personnel with appropriate safety measures.
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| References | |
| Additional Infomation |
(±)-Anatoxin A fumarate (CAS#: 1219922-30-1) is a highly potent, research-grade nicotinic agonist. It is used as a pharmacological probe to study nAChR function, cholinergic signaling, and neurotoxicity mechanisms. Its high affinity for α4β2 nAChRs makes it a key tool for receptor studies.
|
| Molecular Formula |
C14H19NO5
|
|---|---|
| Molecular Weight |
281.30
|
| Exact Mass |
281.126
|
| CAS # |
1219922-30-1
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| PubChem CID |
45073416
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| Appearance |
Light yellow to yellow ointment
|
| LogP |
1.456
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
20
|
| Complexity |
351
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=O)C1=CCCC2CCC1N2.C(=C\C(=O)O)/C(=O)O
|
| InChi Key |
ZJSIFVODFDHYJU-WLHGVMLRSA-N
|
| InChi Code |
InChI=1S/C10H15NO.C4H4O4/c1-7(12)9-4-2-3-8-5-6-10(9)11-8;5-3(6)1-2-4(7)8/h4,8,10-11H,2-3,5-6H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
|
| Chemical Name |
1-(9-azabicyclo[4.2.1]non-2-en-2-yl)ethanone;(E)-but-2-enedioic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5549 mL | 17.7746 mL | 35.5492 mL | |
| 5 mM | 0.7110 mL | 3.5549 mL | 7.1098 mL | |
| 10 mM | 0.3555 mL | 1.7775 mL | 3.5549 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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