| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
IC50: 0.5 nM (α3β2)[1].
α-Conotoxin MII targets the α3β2 subunit of nicotinic acetylcholine receptors (nAChRs). It is a highly potent and selective competitive antagonist for these receptors. It exhibits an IC50 of 0.5-3.5 nM at α3β2 expressed in Xenopus oocytes. It is also an effective inhibitor of β3-containing nAChRs. |
|---|---|
| ln Vitro |
In oocytes expressing α3β2 nicotinic acetylcholine receptors, α-Conotoxin MII (0.5-3.5 nM) stops ACh responses[1][2].
In vitro, α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 nAChRs, with an IC50 of 0.5-3.5 nM. It is used as a powerful pharmacological tool to study the function of α3β2 nAChRs, which are involved in neurotransmitter release and other neuronal processes. |
| ln Vivo |
In vivo, α-Conotoxin MII is not typically used as a therapeutic agent. Its potent and selective antagonism of α3β2 nAChRs makes it a valuable research tool for understanding the role of these receptors in various physiological processes, including pain, addiction, and neurodegeneration. Its use is primarily in research settings.
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| Enzyme Assay |
Non-cell-based assays for α-Conotoxin MII involve radioligand binding displacement studies using membrane preparations from cells expressing α3β2 nAChRs. A radiolabeled ligand, such as [125I]-α-conotoxin MII, is used. The binding affinity and selectivity of the compound are determined by its ability to displace the radiolabeled ligand.
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| Cell Assay |
For in vitro cellular assays, Xenopus oocytes or mammalian cell lines expressing α3β2 nAChRs are used. The compound's antagonistic activity is assessed using electrophysiological techniques like two-electrode voltage clamp. The reduction in acetylcholine-evoked currents in the presence of α-Conotoxin MII is measured to determine its IC50 (0.5-3.5 nM).
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| Animal Protocol |
In vivo animal studies with α-Conotoxin MII typically involve administering the peptide to rodents, often via intrathecal injection, to study its effects on pain pathways. Its antagonism of α3β2 nAChRs, which are involved in pain modulation, can help elucidate the role of this receptor subtype in chronic pain conditions.
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| ADME/Pharmacokinetics |
α-Conotoxin MII is a peptide with a molecular weight and formula as provided in its sequence. Its CAS number is 175735-93-0. It is a natural product isolated from cone snail venom. It is typically supplied as a lyophilized powder and should be stored at -20°C. It is for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of α-Conotoxin MII is primarily related to its mechanism of action. As a potent nAChR antagonist, it can be highly toxic, as it is a component of a deadly cone snail venom. It is for research use only and should be handled with extreme caution.
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| References |
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| Additional Infomation |
α-Conotoxin MII (CAS#: 175735-93-0) is a highly specific and potent peptide antagonist for α3β2 nAChRs. It is a critical tool in neuropharmacology for studying the structure, function, and physiological roles of this nAChR subtype. Its high selectivity makes it invaluable for dissecting the contributions of α3β2 receptors in complex neuronal circuits.
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| Molecular Formula |
C67H103N23O22S4
|
|---|---|
| Molecular Weight |
1710.94
|
| Exact Mass |
1709.65
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| CAS # |
175735-93-0
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| PubChem CID |
138630151
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
23
|
| Hydrogen Bond Acceptor Count |
29
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
116
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| Complexity |
3540
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| Defined Atom Stereocenter Count |
0
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5845 mL | 2.9224 mL | 5.8447 mL | |
| 5 mM | 0.1169 mL | 0.5845 mL | 1.1689 mL | |
| 10 mM | 0.0584 mL | 0.2922 mL | 0.5845 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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