| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| 10mg | ||
| Other Sizes |
| Targets |
Neuronal Sodium Channels (NaV) (slows inactivation)
|
|---|---|
| ln Vitro |
β-Pompilidotoxin (β-PMTX) causes resurgent current in med neurons and increases it in wild-type neurons. In wild-type Purkinje cells, β-Pompilidotoxin (10 μM) slightly but significantly enhanced the decay time constant (τdecay) of currents elicited by a step from -90 to 0 mV from 0.52 to 0.73 msec[1].
beta-Pompilidotoxin (beta-PMTX) slows sodium channel inactivation and increases steady-state sodium current in cells. It facilitates neuromuscular synaptic transmission. The toxin is selective for rat neuronal sodium channel alpha-subunits over cardiac sodium channel alpha-subunits, making it a tool to study neuronal excitability and synaptic transmission. In vitro, beta-PMTX increases resurgent current in wild-type neurons and induces resurgent current in med neurons. |
| ln Vivo |
No specific in vivo data available. As a wasp venom neurotoxin, it is not used therapeutically in vivo but rather as a pharmacological tool to dissect sodium channel function in neuronal systems. It facilitates neurotransmitter release at neuromuscular junctions and can be used to study pain pathways or synaptic plasticity when injected locally or applied in brain slice preparations.
|
| Enzyme Assay |
For binding assays, rat brain synaptosomes or purified sodium channel preparations are used. Radioligand binding with [3H]saxitoxin or [3H]batrachotoxin can be performed to assess allosteric modulation. Alternatively, electrophysiological assays are more common. beta-Pompilidotoxin is applied to voltage-clamped neurons, and its effect on the rate of sodium channel inactivation is measured by analyzing the decay of macroscopic sodium currents. The toxin slows the inactivation time constant (τ).
|
| Cell Assay |
Primary cultured rat dorsal root ganglion (DRG) neurons or hippocampal neurons are used. Cells are cultured in Neurobasal medium with B27 supplement and growth factors. Whole-cell patch-clamp recordings are performed. Sodium currents are elicited by depolarizing voltage steps from a negative holding potential. beta-Pompilidotoxin (0.1-10 uM) is applied, and the effect on current decay kinetics (inactivation) is measured. The toxin slows inactivation, leading to increased persistent/resurgent currents. The toxin can also be applied to brain slices to study synaptic transmission.
|
| Animal Protocol |
No published in vivo animal study for beta-Pompilidotoxin. For assessment of toxin effects in vivo, beta-Pompilidotoxin could be injected into the hind paw of mice (0.1-10 ug) to study pain behavior (nociception) or into the cerebrospinal fluid (intrathecal injection) to study central effects. However, the primary application is ex vivo or in vitro. Wasps use the toxin to paralyze prey (insects) by disrupting neuromuscular transmission, so insect models could be used.
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Free toxins can be cleared through opsonization by the reticuloendothelial system (mainly in the liver and kidneys) and degraded through endocytosis by lysosomes. Lysosomes are membrane-bound organelles containing various digestive enzymes, including several proteases. No specific PK data for beta-Pompilidotoxin. As a peptide (MW ~1557.88 Da, 13 amino acids), it is not orally bioavailable and would be degraded by proteases in vivo. For research, it is typically applied directly to tissues or injected. It is soluble in water or saline. The toxin is stable when stored as a lyophilized powder at -20degC or -80degC. For long-term storage, avoid repeated freeze-thaw cycles. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Pompilide can slow the inactivation of neuronal sodium channels (but not cardiac sodium channels), thereby enhancing synaptic transmission. Its mechanism of action is believed to be through binding to neurotoxin receptor site 3 on the extracellular surface of sodium channels. (L1018, A309) No specific toxicity data for beta-Pompilidotoxin. As a peptide toxin, it can cause neurotoxicity by altering sodium channel function, leading to hyperexcitability, muscle spasms, and paralysis. In vivo toxicity would be dose-dependent. For research use, handle with extreme caution: avoid inhalation, skin contact, and self-injection. Wear gloves and lab coat. The toxin may be lethal if injected systemically in small animals. |
| References |
[1]. Tina M Grieco, et al. Production of resurgent current in NaV1.6-null Purkinje neurons by slowing sodium channel inactivation with beta-pompilidotoxin. J Neurosci. 2004 Jan 7;24(1):35-42.
|
| Additional Infomation |
There have been reports that β-pompidol toxin has been detected in the Shamari ant, and relevant data are available for reference.
beta-Pompilidotoxin (CAS: 216064-36-7) is a 13-amino acid peptide neurotoxin from wasp venom (sequence: Arg-Gly-Ile-Asp-Phe-Gln-Gly-Lys-Tyr-Ala-Met-Gly-Ser-NH2, MW 1557.88). It is used as a research tool to study voltage-gated sodium channels, particularly the role of channel inactivation in neuronal excitability. It is also known as beta-PMTX. The toxin facilitates neuromuscular transmission by slowing Na+ channel inactivation. It is sold as a research reagent only; not for human use. References: Konno K, et al. (1996). |
| Molecular Formula |
C71H124N22O17
|
|---|---|
| Molecular Weight |
1557.88
|
| Exact Mass |
1556.95
|
| CAS # |
216064-36-7
|
| PubChem CID |
90479801
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.983
|
| Hydrogen Bond Donor Count |
22
|
| Hydrogen Bond Acceptor Count |
21
|
| Rotatable Bond Count |
55
|
| Heavy Atom Count |
110
|
| Complexity |
3070
|
| Defined Atom Stereocenter Count |
14
|
| SMILES |
NCCCC[C@@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(=O)N)CC(C)C)=O)CCC/N=C(\N)/N)=O)CO)=O)CC(C)C)=O)CCC(=O)N)=O)CC(=O)O)=O)CC1C=CC=CC=1)=O)CC(C)C)=O)=O)[C@H](CC)C)=O)NC([C@H]([C@H](CC)C)NC([C@H](CCC/N=C(\N)/N)N)=O)=O
|
| InChi Key |
YBOJYGJMKPMNRC-QRIWDNSUSA-N
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| InChi Code |
InChI=1S/C71H124N22O17/c1-11-40(9)56(93-62(103)44(23-16-17-27-72)86-69(110)57(41(10)12-2)92-59(100)43(73)22-18-28-80-70(76)77)68(109)82-35-54(96)83-48(31-38(5)6)63(104)89-50(33-42-20-14-13-15-21-42)65(106)90-51(34-55(97)98)66(107)85-46(25-26-53(74)95)61(102)88-49(32-39(7)8)64(105)91-52(36-94)67(108)84-45(24-19-29-81-71(78)79)60(101)87-47(58(75)99)30-37(3)4/h13-15,20-21,37-41,43-52,56-57,94H,11-12,16-19,22-36,72-73H2,1-10H3,(H2,74,95)(H2,75,99)(H,82,109)(H,83,96)(H,84,108)(H,85,107)(H,86,110)(H,87,101)(H,88,102)(H,89,104)(H,90,106)(H,91,105)(H,92,100)(H,93,103)(H,97,98)(H4,76,77,80)(H4,78,79,81)/t40-,41-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,56-,57-/m0/s1
|
| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylpentanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-4-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-oxobutanoic acid
|
| 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)
|
| Solubility (In Vitro) |
H2O: ≥ 100 mg/mL (64.19 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 | 0.6419 mL | 3.2095 mL | 6.4190 mL | |
| 5 mM | 0.1284 mL | 0.6419 mL | 1.2838 mL | |
| 10 mM | 0.0642 mL | 0.3209 mL | 0.6419 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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