| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In the presence of EC5 GABA at α1β2γ2L GABAA receptors, picrotoxinin (0.001 μM-1 mM; 60-90 s) suppresses the activity of GABAA receptors and modifies GABAA modulators [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: Xenopus laevis oocytes Tested Concentrations: 0.001 µM-1 mM Incubation Duration: 60 and 90 seconds Experimental Results: Dose-dependent inhibition of GABAA receptors, IC50 is 1.15 µM, comparable to similar drugs demonstrated the strongest activity than bilobalide and ginkgolide B. Inhibition of etomidate, propofol, diazepam, thiopental, lorracozole and isopropanol at α1β2γ2L GABAA receptors in the presence of EC5 GABA Progesterone, IC50 is 0.55, 0.49, 0.35-0.36, 0.50, 0.14 and 0.44 μM respectively. |
| References |
[1]. Ng CC, et al. Effects of bilobalide, ginkgolide B and picrotoxinin on GABAA receptor modulation by structurally diverse positive modulators. Eur J Pharmacol. 2017 Jul 5;806:83-90.
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| Molecular Formula |
C15H16O6
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|---|---|
| Molecular Weight |
292.29
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| Exact Mass |
292.0947
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| CAS # |
17617-45-7
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| Related CAS # |
Picrotoxin;124-87-8
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
C=C(C)C1[C@@H]2C(=O)O[C@H]1[C@@H]3[C@]4(C)[C@]2(C[C@@H]5[C@@]4(C(=O)O3)O5)O
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| Synonyms |
NSC-129537; NSC 129537; Picrotoxinin
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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 (~342.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4213 mL | 17.1063 mL | 34.2126 mL | |
| 5 mM | 0.6843 mL | 3.4213 mL | 6.8425 mL | |
| 10 mM | 0.3421 mL | 1.7106 mL | 3.4213 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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