| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
ecdysone receptor[2]
Ecdysone receptor. It has a strong affinity for ecdysone receptors, making it a potent regulator of gene expression in cells and transgenic animals. |
|---|---|
| ln Vitro |
In CV-1 cells, ponasterone A (1 nM-100 μM) significantly activates genes [2].
In vitro, Ponasterone A shows significant gene induction activity in CV-1 cells, with an EC50 of 0.07 µM. It induces expression of reporter genes (e.g., beta-galactosidase) to levels similar to those obtained with other potent ecdysteroids like muristerone A. |
| ln Vivo |
In transactivator and reporter mice, ponasterone A (3–10 mg; i.p.) significantly increases gene expression [2].
In vivo, Ponasterone A (3-10 mg; i.p.) produces robust inductions of gene expression in transactivator and reporter mice. It is a potent regulator of gene expression in transgenic animals, enabling reporter genes to be rapidly turned on and off. |
| Enzyme Assay |
A standard in vitro assay uses CV-1 cells transfected with an ecdysone-inducible reporter system. Cells are treated with varying concentrations of Ponasterone A (e.g., 1 nM-100 µM) for a defined period, and reporter gene activity (e.g., luciferase) is measured to generate a dose-response curve and determine the EC50.
|
| Cell Assay |
The gene-inducing activity of Ponasterone A is assessed in cell lines (e.g., CV-1) that have been engineered to express the ecdysone receptor and a reporter gene under the control of an ecdysone-responsive promoter. Cells are treated with the compound, and the level of reporter gene expression is quantified to measure the compound's potency.
|
| Animal Protocol |
In vivo activity is evaluated in transgenic mice that carry both the ecdysone receptor and a reporter gene. Ponasterone A is administered via intraperitoneal injection, and the induction of the reporter gene is measured in various tissues to assess the compound's bioavailability and efficacy in different organs.
|
| ADME/Pharmacokinetics |
Ponasterone A is a small molecule (MW 464.64) that is soluble in organic solvents like DMSO, ethanol, and methanol but insoluble in water. Its pharmacokinetics are characterized by its ability to cross cell membranes and reach its intracellular receptor. It is typically used as an inducer in research settings.
|
| Toxicity/Toxicokinetics |
Ponasterone A is considered non-toxic to vertebrates at the concentrations used for gene induction. This makes it a safe and effective tool for regulating gene expression in mammalian systems. Specific toxicity data are available in its safety data sheet.
|
| References | |
| Additional Infomation |
Ponasterone A is a 2β-hydroxysterol, 3β-hydroxysterol, 14α-hydroxysterol, 20-hydroxysterol, 22-hydroxysterol, 6-oxosterol, and phytoecdysterol. It has been reported to be found in yew (Taxus cuspidata), Douglas marsh tree (Limnanthes douglasii), and other organisms with relevant data.
Ponasterone A is a key tool in the field of chemical genetics and gene therapy research. Its high potency and low toxicity in mammals make it an ideal inducer for the ecdysone-inducible expression system, which allows for precise, temporal, and dose-dependent control of gene expression in cells and animals. |
| Molecular Formula |
C27H44O6
|
|---|---|
| Molecular Weight |
464.63
|
| Exact Mass |
464.313
|
| CAS # |
13408-56-5
|
| PubChem CID |
115127
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
640.5±55.0 °C at 760 mmHg
|
| Flash Point |
355.2±28.0 °C
|
| Vapour Pressure |
0.0±4.3 mmHg at 25°C
|
| Index of Refraction |
1.582
|
| LogP |
1.55
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
33
|
| Complexity |
823
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
O([H])[C@@]12C([H])([H])C([H])([H])[C@]([H])([C@](C([H])([H])[H])([C@@]([H])(C([H])([H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])O[H])O[H])[C@@]1(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]1([H])C2=C([H])C([C@]2([H])C([H])([H])[C@]([H])([C@]([H])(C([H])([H])[C@]12C([H])([H])[H])O[H])O[H])=O
|
| InChi Key |
PJYYBCXMCWDUAZ-JJJZTNILSA-N
|
| InChi Code |
InChI=1S/C27H44O6/c1-15(2)6-7-23(31)26(5,32)22-9-11-27(33)17-12-19(28)18-13-20(29)21(30)14-24(18,3)16(17)8-10-25(22,27)4/h12,15-16,18,20-23,29-33H,6-11,13-14H2,1-5H3/t16-,18-,20+,21-,22-,23+,24+,25+,26+,27+/m0/s1
|
| Chemical Name |
(2S,3R,5R,9R,10R,13R,14S,17S)-17-[(2R,3R)-2,3-dihydroxy-6-methylheptan-2-yl]-2,3,14-trihydroxy-10,13-dimethyl-2,3,4,5,9,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-6-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO: 100 mg/mL (215.23 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 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 (5.38 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 (5.38 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 | 2.1523 mL | 10.7613 mL | 21.5225 mL | |
| 5 mM | 0.4305 mL | 2.1523 mL | 4.3045 mL | |
| 10 mM | 0.2152 mL | 1.0761 mL | 2.1523 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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