| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
alpha7 nicotinic acetylcholine receptor (alpha7 nAChR). Also binds to muscle‑type nAChRs at the neuromuscular junction with extremely high affinity (Kd 1 nM to 1 pM). Does not bind alpha4beta2 nAChRs. IC50 for alpha7 is ~1.6 nM, with no effect on alpha3beta4 up to 3 microM.
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| ln Vitro |
α-Bungarotoxin exhibits high affinity and selective binding to the nicotinic acetylcholine receptor, hence competing with natural ligand binding. Because it functionally blocks AcChoRs at the neuromuscular junction, α-Bungarotoxin (α-BTX) is a very lethal competitive inhibitor of nicotinic acetylcholine receptor function[3].
In vitro, alpha‑Bungarotoxin blocks alpha7 nAChR‑mediated currents with IC50 = 1.6 nM. It inhibits nicotine‑induced Ca2+ rise in PC12 cells (IC50 = 310 nM). It acts postsynaptically, not affecting acetylcholine release. In frog rectus abdominis, it blocks neuromuscular transmission by preventing receptor activation. |
| ln Vivo |
In vivo, the toxin is highly lethal due to irreversible blockade of neuromuscular nAChRs. Mouse LD50 values: 0.108 mg/kg (s.c.), 0.113 mg/kg (i.v.), 0.08 mg/kg (i.p.). It causes progressive muscle paralysis starting from face and neck, leading to respiratory failure. Does not cross the blood‑brain barrier. No therapeutic use.
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| Enzyme Assay |
Use rat brain cortical membranes (10‑20 microg protein). Incubate with 0.5‑1 nM [¹2⁵I]‑alpha‑Bungarotoxin and 0.01‑1000 nM unlabeled toxin in 50 mM Tris‑HCl pH 7.4 with 0.1% BSA for 2‑3 h at room temp. Non‑specific binding determined with 10 microM unlabeled alpha‑Bungarotoxin or 1 mM nicotine. Harvest by rapid filtration through PEI‑soaked GF/B filters, wash 3×, count gamma radiation. Calculate Ki from IC50 via Cheng‑Prusoff.
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| Cell Assay |
Seed PC12 cells in poly‑D‑lysine 96‑well plates (50,000/well) in RPMI/10% horse serum/5% FBS for 48 h. Load cells with 2.5 microM Fluo‑4 AM in HBSS/HEPES/probenecid for 60 min at 37degC. Wash, then pre‑incubate with alpha‑Bungarotoxin (0.01‑10 microM) for 30 min. Add 30 microM nicotine to stimulate Ca2+ influx. Measure fluorescence (ex/em 485/525 nm). Determine IC50 for inhibition of the Ca2+ response.
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| Animal Protocol |
Use male CD‑1 mice (20‑30 g). Inject alpha‑Bungarotoxin i.p., i.v., or s.c. at 0.01‑0.2 mg/kg. For neuromuscular blockade, anesthetize and stimulate sciatic nerve while recording gastrocnemius twitch. Administer toxin i.v. (0.01‑0.05 mg/kg) and measure time to 50% twitch reduction (T50). Monitor up to 72 h for LD50 (paralysis, respiratory distress, death).
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| ADME/Pharmacokinetics |
Peptide of ~8 kDa. Does not cross BBB. Plasma t½ in rodents ~1‑2 h. Cleared by renal filtration and proteolysis. Not orally bioavailable. Rapidly distributes to neuromuscular junctions and peripheral nAChR‑expressing tissues. No active metabolites. Excreted in urine as degraded fragments.
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| Toxicity/Toxicokinetics |
Extremely potent neurotoxin. Mouse LD50 i.p. = 0.08 mg/kg. Mechanism: irreversible competitive blockade of nAChRs at neuromuscular junction → paralysis of respiratory muscles → death. No antidote; supportive ventilation required. Signs appear within minutes. Strictly for research, not for human use.
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| References |
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| Additional Infomation |
Used exclusively as a research tool to map alpha7 nAChRs. Competitive antagonist that binds orthosteric site. Not approved for any clinical indication. Often radiolabeled for autoradiography. CAS 11032‑79‑4. Handle with extreme caution in a laboratory setting. No clinical trials or therapeutic applications.
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| Molecular Formula |
C50H70O14
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|---|---|
| Molecular Weight |
895.082400000001
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| CAS # |
11032-79-4
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| Appearance |
White to off-white solid powder
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| SMILES |
O=CC(C[C@H]1C[C@H](O)[C@@]2(O[C@@H]3C[C@@H]4O[C@@H]5C[C@@]6(O[C@@]7(CC[C@@H]8O[C@@H]9C[C@]%10(C)O[C@@H]%11C(C)=CC(=O)O[C@H]%11C[C@H]%10O[C@H]9C[C@@H](C)[C@H]8O[C@H]7C[C@H]6O[C@@]5(C)CC=C[C@H]4O[C@H]3C[C@H]2O1)C)C)C)=C |c:59,&1:4,6,8,10,12,14,16,18,21,23,25,28,35,37,39,41,43,45,47,49,54,56,58|
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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) |
H2O: ≥ 50 mg/mL (6.26 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 | 1.1172 mL | 5.5861 mL | 11.1722 mL | |
| 5 mM | 0.2234 mL | 1.1172 mL | 2.2344 mL | |
| 10 mM | 0.1117 mL | 0.5586 mL | 1.1172 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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