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5mg |
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25mg |
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50mg |
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Purity: ≥98%
20-Hydroxyecdysone (also known as B-ecdysone, Crustecdysone, Commisterone Ecdysterone, 20E) is an ecdysteroid hormone that is present in nature and regulates the ecdysis (moulting) and metamorphosis of arthropods. In H4IIE cell culture, 20-Hydroxyecdysone treatment reduces the expression of the enzymes glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK), lowers glucose production, and increases Akt2 phosphorylation that is responsive to the phosphoinositide-3 kinase pathway inhibitor LY-294002. Treatment with 20-hydroxyecdysone either before or after exposure to CoCl2 significantly reduces CoCl2-induced cellular damage.
Targets |
Human Endogenous Metabolite
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ln Vitro |
20-Hydroxyecdysone treatment in H4IIE cell culture reduces the expression of glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK), lowers glucose production, and increases Akt2 phosphorylation sensitive to the phosphoinositide-3 kinase pathway-specific inhibitor LY-294002.[1] Treatment with 20-hydroxyecdysone either before or after exposure to CoCl2 significantly lessens the cellular damage caused by CoCl2. 20-Hydroxyecdysone significantly decreases the production of reactive oxygen species (ROS) that CoCl2-induced, as well as the depolarization of the mitochondrial membrane, the release of cytochrome c into the cytosol, the Bax/Bcl-2 ratio, and the activation of caspase-3 that CoCl2-induced.[2] With an IC50 of 31.8 µM, 20-hydroxyecdysone prevents NF-κB activation in HeLa cells that have been persistently transfected with an IL-6-bound reporter gene.[3] The apoptotic genes Apaf-1, Nedd2 like1, Nedd2 like2, ICE1, ICE3, ICE5, Arp, and IAP are upregulated when 20-Hydroxyecdysone is administered to larval fat body tissues in vitro.[4] 20-hydroxyecdysone reverses TGF-1-induced upregulation of Smad7 and upregulation of intracellular and extracellular fibronectin. 20-Hydroxyecdysone also significantly reduces the effects of TGF-1 on the upregulation of Smad2/3 and pSmad2/3, as well as the downregulation of E-Cadherin. Additionally, TGF-1-induced increases in Snail expression are sharply suppressed by 20-hydroxyecdysone.[5]
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ln Vivo |
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Enzyme Assay |
Ingested ecdysteroids (20E or E) reach a plasma titre maximum after ca. 30 min in humans and sheep and are rapidly cleared from the blood and urine, but the proportions of the applied dose found in these are very low, accounting only for a few percent. The effective half-time of elimination from the blood in humans was found to be 4 h for E and 9 h for 20E, and 3.1 h for E and 3.3 h for 20E for elimination from the urine[7].
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Cell Assay |
Methods:[5]
The proximal tubular epithelial cells (designated as HK-2) were treated for 48 h with TGF-β1 (5 ng/ml) in different concentrations of 20-HE (0 to 500 nM/ml) in the last 24 h of culture. The extracellular fibronectin was measured by ELISA assay. Western blot and immunofluorescence were used to evaluate the expression of TGF-β1/Smads transducer (including Smad2/3, 4, and 7), epithelial and mesenchymal markers (e.g. E-cadherin and α-smooth muscle actin) and Snail (transcriptional regulators for EMT). Results:[5] 20-HE reverses TGF-β1-induced increase in fibronectin (both intracellular and extracellular fibronectin). Simultaneously, 20-HE reverses TGF-β1-induced down-regulation of Smad7. In addition, 20-HE significantly attenuates TGF-β1-induced upregulation of Smad2/3 and pSmad2/3, and downregulation of E-Cadherin. Moreover, 20-HE dramatically suppresses TGF-β1-induced increases in the expression of Snail. |
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Animal Protocol |
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References |
[1]. Am J Physiol Endocrinol Metab. 2009 Mar;296(3):E433-9. [2]. J Cell Biochem. 2010 Dec 15;111(6):1512-21. doi: 10.1002/jcb.22877. [3]. J Pharm Pharmacol. 2011 Nov;63(11):1483-95. [4]. Arch Insect Biochem Physiol. 2012 Apr;79(4-5):207-19. [5]. J Diabetes Complications. 2012 Nov-Dec;26(6):463-9. |
Molecular Formula |
C27H44O7
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Molecular Weight |
480.63
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Exact Mass |
480.3087
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Elemental Analysis |
C, 67.47; H, 9.23; O, 23.30
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CAS # |
5289-74-7
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Related CAS # |
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Appearance |
White to off-white solid powder
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Source |
Serratula coronata
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LogP |
-0.53
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tPSA |
138.45
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SMILES |
C[C@]12CC[C@H]3C(=CC(=O)[C@H]4[C@@]3(C[C@@H]([C@@H](C4)O)O)C)[C@@]1(CC[C@@H]2[C@](C)([C@@H](CCC(C)(C)O)O)O)O
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InChi Key |
NKDFYOWSKOHCCO-YPVLXUMRSA-N
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InChi Code |
InChI=1S/C27H44O7/c1-23(2,32)9-8-22(31)26(5,33)21-7-11-27(34)16-12-18(28)17-13-19(29)20(30)14-24(17,3)15(16)6-10-25(21,27)4/h12,15,17,19-22,29-34H,6-11,13-14H2,1-5H3/t15-,17-,19+,20-,21-,22+,24+,25+,26+,27+/m0/s1
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Chemical Name |
(2S,3R,5R,9R,10R,13R,14S,17S)-2,3,14-trihydroxy-10,13-dimethyl-17-[(2R,3R)-2,3,6-trihydroxy-6-methylheptan-2-yl]-2,3,4,5,9,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-6-one
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Synonyms |
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.33 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 20.8 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: ≥ 2.08 mg/mL (4.33 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 20.8 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: ≥ 2.08 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 30 mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0806 mL | 10.4030 mL | 20.8060 mL | |
5 mM | 0.4161 mL | 2.0806 mL | 4.1612 mL | |
10 mM | 0.2081 mL | 1.0403 mL | 2.0806 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04827537 | Active Recruiting |
Drug: Placebo Oral Drug: Metronidazole Oral |
Giardia Lamblia Infection | Research Institute of Epidemiology, Microbiology and Infectious Diseases, Uzbekistan |
January 1, 2021 | Phase 2 Phase 3 |
NCT03452488 | Completed | Drug: BIO101 Drug: Placebo oral capsule |
Sarcopenia Muscle Weakness |
Biophytis | May 24, 2018 | Phase 2 |
20-Hydroxyecdysone. Phytother Res . 2013 Jan;27(1):107-11. td> |