| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Neuronal nicotinic acetylcholine receptors (nAChRs). Selectively antagonizes alpha7 nAChR (IC50 = 7.9 nM) and also blocks alpha3beta2-containing nAChRs. The peptide is a competitive antagonist that binds to the orthosteric site of the receptor.
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| ln Vitro |
alpha-Conotoxin PnIA selectively antagonizes alpha7 nAChRs with an IC50 of 7.9 nM and alpha3beta2 nAChRs with an IC50 of 62.7 nM. It is a competitive antagonist that binds to the orthosteric acetylcholine binding site. Its high selectivity for mammalian alpha7 nAChRs makes it valuable for studying this receptor's role in synaptic plasticity, neuroprotection, and inflammation.
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| ln Vivo |
In vivo, alpha-Conotoxin PnIA (0.1 nmol/kg) in combination with baicalein has been studied in animal models of neuropathic pain and Alzheimer's disease. It may reduce pain behaviors, improve cognitive function, and modulate neuroinflammatory responses in rodent models. Further studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
For binding assays, rat brain membranes or cells expressing nAChR subtypes are incubated with radiolabeled alpha-conotoxin PnIA (e.g., 125I-labeled) or a radiolabeled competitor (e.g., 125I-alpha-bungarotoxin). Increasing concentrations of unlabeled PnIA (0.1-1000 nM) are added to displace the radioligand. Bound radioactivity is measured by scintillation counting, and IC50 values are calculated.
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| Cell Assay |
For functional assays, cells expressing nAChRs (e.g., Xenopus oocytes injected with nAChR subunit cRNAs) are voltage-clamped. alpha-Conotoxin PnIA (0.1-1000 nM) is applied, and acetylcholine (ACh)-evoked currents are measured. The percentage inhibition of ACh-evoked currents is plotted against toxin concentration to calculate IC50 values. For neuronal cultures, calcium influx via nAChRs is measured using calcium-sensitive dyes (e.g., Fluo-4) with ACh stimulation.
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| Animal Protocol |
For animal studies, alpha-Conotoxin PnIA is administered intrathecally (for pain studies), intravenously, or intracerebroventricularly to rodent models (e.g., neuropathic pain induced by nerve injury or Alzheimer's models). Doses typically range from 0.1-10 nmol/kg. Pain behavior (von Frey test, hot plate test) is assessed, and cognitive function is evaluated using Morris water maze or novel object recognition. Tissues are collected for immunohistochemistry and biochemical analysis.
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| ADME/Pharmacokinetics |
alpha-Conotoxin PnIA is a peptide, so its oral bioavailability is poor. It is typically administered via injection (i.v., i.t., i.c.v.). The half-life in vivo is short (minutes to hours) due to rapid proteolytic degradation and clearance. For research use, it is often formulated in saline or PBS. It is stable in lyophilized form at -20degC for long-term storage.
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| Toxicity/Toxicokinetics |
Toxicity data for alpha-Conotoxin PnIA are limited to research studies. At therapeutic doses (0.1-10 nmol/kg in animal models), no significant systemic toxicity has been reported. High doses may cause receptor-mediated toxicity related to excessive nAChR blockade. As a peptide neurotoxin, standard precautions for handling animal-derived toxins should be observed.
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| References | |
| Additional Infomation |
alpha-Conotoxin PnIA TFA has the molecular formula C65H95N19O22S4 and molecular weight 1622.8. The amino acid sequence is GCCSLPPCAANNPDYC-NH2 with disulfide bonds between Cys2-Cys8 and Cys3-Cys16. It is a valuable tool for studying nAChR function in neurological disorders. It is not approved for clinical use and is intended for research applications only.
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| Molecular Formula |
C67H96F3N19O24S4
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| Molecular Weight |
1736.82
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| Appearance |
White to off-white solid powder
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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 |
| 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) |
DMSO :~100 mg/mL (~57.58 mM)
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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 | 0.5758 mL | 2.8788 mL | 5.7576 mL | |
| 5 mM | 0.1152 mL | 0.5758 mL | 1.1515 mL | |
| 10 mM | 0.0576 mL | 0.2879 mL | 0.5758 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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