| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Neuronal nicotinic acetylcholine receptors (nAChRs). alpha-Conotoxin PIA is a selective antagonist for nAChR subtypes containing the alpha6 subunit (IC50 = 0.95 nM for rat alpha6/alpha3beta2beta3) over alpha3beta2-containing receptors (IC50 = 74.2 nM).
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| ln Vitro |
alpha-Conotoxin PIA potently blocks alpha6-containing nAChRs with an IC50 of 0.95 nM for rat alpha6/alpha3beta2beta3, showing approximately 78-fold selectivity over alpha3beta2 receptors (IC50 = 74.2 nM). It does not block muscle-type nAChRs or the major neuronal alpha4beta2 subtype. This unique selectivity makes it a key tool for studying alpha6* nAChR function.
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| ln Vivo |
In vivo, alpha-Conotoxin PIA has been used to study the role of alpha6-containing nAChRs in dopamine release and motor function, as these receptors are enriched in dopaminergic neurons. It has potential for research into Parkinson's disease (where nigrostriatal dopamine neurons degenerate) and schizophrenia (where dopamine signaling is dysregulated).
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| Enzyme Assay |
For nAChR binding assays, rat brain synaptosomes or cells expressing specific nAChR subunits (e.g., alpha6/alpha3beta2beta3 in Xenopus oocytes) are incubated with alpha-Conotoxin PIA (0.1-1000 nM). Radiolabeled conotoxin or alpha-bungarotoxin is used as a tracer. Bound radioactivity is measured. Alternatively, competitive binding assays with 125I-alpha-conotoxin MII (which also binds alpha6* receptors) can be performed.
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| Cell Assay |
For functional assays (electrophysiology), Xenopus oocytes are injected with cRNAs encoding nAChR subunits (alpha6, alpha3, beta2, beta3). Two-electrode voltage-clamp recordings are performed. ACh-evoked currents are measured before and after application of alpha-Conotoxin PIA (0.1-1000 nM). The percentage inhibition of ACh-evoked currents is plotted to calculate IC50 values for different subunit combinations.
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| Animal Protocol |
For animal studies, alpha-Conotoxin PIA is administered intracerebroventricularly (i.c.v.) or intrathecally to rodent models of Parkinson's disease (e.g., 6-OHDA-lesioned rats) or schizophrenia (e.g., prepulse inhibition models). Doses typically range from 0.01-1 nmol/kg. Dopamine release in the striatum or nucleus accumbens may be measured by microdialysis. Motor function is assessed by rotarod or open field tests. Behavioral assays for sensorimotor gating (prepulse inhibition) may be performed.
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| ADME/Pharmacokinetics |
alpha-Conotoxin PIA is a 19-amino-acid peptide with poor oral bioavailability. For in vivo studies, it is administered via injection (i.c.v., i.t.). The half-life is short due to proteolytic degradation. It is stable in lyophilized form at -20degC for long-term storage. For experimental use, it is typically dissolved in saline or artificial cerebrospinal fluid and used immediately.
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| Toxicity/Toxicokinetics |
alpha-Conotoxin PIA is a peptide neurotoxin that is toxic if injected at high concentrations due to disruption of nAChR-mediated neurotransmission. At research doses (0.01-1 nmol/kg i.c.v.), no significant systemic toxicity has been reported. Standard safety precautions for handling cone snail toxins should be observed, including use of gloves and avoiding injection or ingestion.
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| References | |
| Additional Infomation |
alpha-Conotoxin PIA TFA has the molecular formula C79H125N27O25S4 and approximate molecular weight 1981.3. It is a 19-mer peptide with four disulfide bonds (characteristic of the alpha4/7 conotoxin fold). It is a valuable tool for studying alpha6-containing nAChRs in dopamine signaling, Parkinson's disease, and schizophrenia. It is not approved for clinical use and is intended for research applications only.
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| Molecular Formula |
C85H128F9N27O31S4
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| Molecular Weight |
2323.33
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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 :≥ 250 mg/mL (~107.60 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 | 0.4304 mL | 2.1521 mL | 4.3042 mL | |
| 5 mM | 0.0861 mL | 0.4304 mL | 0.8608 mL | |
| 10 mM | 0.0430 mL | 0.2152 mL | 0.4304 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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