| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Ecdysone targets the ecdysone receptor (EcR), a nuclear receptor that regulates gene expression during insect development. It triggers mineralocorticoid receptor activation and induces cellular apoptosis.
|
|---|---|
| ln Vitro |
Intratumoral medullary collecting duct cells (IMCD) undergo apoptosis when exposed to ecdysone (alpha-ecdysone; 100 nM; for 48 hours) [1]. Inner medullary collecting duct cells (IMCD) express α-smooth muscle actin (SMA), a classic mesenchymal marker, in a dose-dependent manner when exposed to ecdysone (10, 100 nM) for 48 hours. In a dose-dependent way, ecdysone upregulates the expression of cleaved caspase 3 [1]. A significant amount of cell motility and scratch wound closure is inhibited by ecdysone (10, 100 nM; for 12 24 hours) [1]. Branching spindle mesenchymal-like cell morphologies are induced by 24 and 48 hours of treatment with 100 nM ecdysone [1].
In vitro, ecdysone is used as an ecdysone receptor agonist to study insect development and molting. It triggers mineralocorticoid receptor activation and induces apoptosis in various cell lines. |
| ln Vivo |
Ecdysone (alpha-ecdysone; 6 µg/g/day; SC; for 14 days) markedly reduces renal function as evidenced by a statistically significant rise in BUN levels and amplification of α-SMA expression in the kidneys of male C57BL/6 mice aged 10 weeks. The nephrotic effects of ecdysone are MR-dependent [1].
In vivo, ecdysone is the major steroid hormone that controls molting and development in insects. It is also found in some plants and is believed to have a similar function. It has been studied for its potential role in drug development. |
| Enzyme Assay |
In vitro receptor binding assays for ecdysone typically use membrane preparations or nuclear extracts from insect cells expressing ecdysone receptors. Radiolabeled ecdysteroids are displaced by increasing concentrations of the compound to determine binding affinity. Functional assays measure the compound's ability to activate ecdysone receptor-mediated transcription.
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: Inner medullary collecting duct cells (IMCD) Tested Concentrations: 100 nM Incubation Duration: 48 hrs (hours) Experimental Results: Caused apoptosis of renal tubular cells. Western Blot Analysis[1] Cell Types: IMCD Cell Tested Concentrations: 10, 100 nM Incubation Duration: 48 hrs (hours) Experimental Results: Induces expression of alpha-smooth muscle actin (SMA), a standard mesenchymal Mark. Cell-based assays for ecdysone involve treating insect cell lines with the compound and measuring ecdysone receptor-mediated transcriptional activity. Cells transfected with an ecdysone-responsive reporter gene are treated with varying concentrations of the compound. Reporter gene activity is measured. EC₅₀ values are calculated. |
| Animal Protocol |
In vivo insect studies for ecdysone involve administering the compound to insects and observing its effects on molting and development. The compound's ability to trigger molting and regulate gene expression is assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of ecdysone are characteristic of steroid hormones. The compound has a molecular weight of 464.6 g/mol and a molecular formula of C₂₇H₄₄O₆. It is a steroidal prohormone.
|
| Toxicity/Toxicokinetics |
Ecdysone is generally considered to have low toxicity in mammals. It is a natural hormone with a well-characterized safety profile. High doses may cause hormonal effects.
|
| References |
|
| Additional Infomation |
Ecdysone is a 6-oxosteroid compound with the structure 5β-cholest-7-en-6-one, substituted with hydroxyl groups at positions 2, 3, 14, 22, and 25 (2β, 3β, 22R stereoisomers). It is a precursor hormone of 20-hydroxyecdysone, the major ecdysone in insects, and functions as a precursor hormone. It is a 2β-hydroxysteroid, 14α-hydroxysteroid, 22-hydroxysteroid, 25-hydroxysteroid, 6-oxosteroid, 3β-sterol, and ecdysone compound. It is derived from the hydride of 5β-cholestane. Ecdysone has been reported in Japanese newts, Sichuan yellow-flowered salamanders, and other organisms with relevant data. It is a steroid hormone that regulates the molting process in insects.
Ecdysone is a major insect steroid hormone used as a research tool for studying insect development, molting, and nuclear receptor signaling. It is not approved for therapeutic use. The compound is valuable for investigating the role of ecdysteroids in development and physiology. |
| Molecular Formula |
C27H44O6
|
|---|---|
| Molecular Weight |
464.63466
|
| Exact Mass |
464.314
|
| CAS # |
3604-87-3
|
| PubChem CID |
19212
|
| Appearance |
White to off-white solid powder
|
| Density |
1.22g/cm3
|
| Boiling Point |
632ºC at 760mmHg
|
| Melting Point |
242°C
|
| Flash Point |
350ºC
|
| Index of Refraction |
1.582
|
| LogP |
2.739
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
33
|
| Complexity |
821
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C[C@@H]([C@H]1CC[C@@]2([C@@]1(CC[C@H]3C2=CC(=O)[C@H]4[C@@]3(C[C@@H]([C@@H](C4)O)O)C)C)O)[C@@H](CCC(C)(C)O)O
|
| InChi Key |
UPEZCKBFRMILAV-JMZLNJERSA-N
|
| InChi Code |
InChI=1S/C27H44O6/c1-15(20(28)8-9-24(2,3)32)16-7-11-27(33)18-12-21(29)19-13-22(30)23(31)14-25(19,4)17(18)6-10-26(16,27)5/h12,15-17,19-20,22-23,28,30-33H,6-11,13-14H2,1-5H3/t15-,16+,17-,19-,20+,22+,23-,25+,26+,27+/m0/s1
|
| Chemical Name |
(2S,3R,5R,9R,10R,13R,14S,17R)-17-[(2S,3R)-3,6-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 |
| 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 : ~50 mg/mL (~107.61 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.69 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 12.5 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: ≥ 1.25 mg/mL (2.69 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 12.5 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: ≥ 1.25 mg/mL (2.69 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.