| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
11beta-HSD1 (indirect); glucocorticoid receptor (via corticosterone). 11-Dehydrocorticosterone is the inert 11-keto form of corticosterone. It is converted to active corticosterone by 11beta-HSD1, which is expressed in many tissues. Corticosterone then binds to and activates the glucocorticoid receptor (GR). Thus, the compound acts as a reservoir for active glucocorticoids. It is also a substrate for 11beta-HSD2, which converts it further. Chronic administration increases plasma glucocorticoid levels, body weight, adiposity, and induces insulin resistance in mice.
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| ln Vitro |
11-Dehydrocorticosterone increases SGK mRNA expression in cardiac fibroblasts. As a glucocorticoid metabolite, it is converted to active corticosterone by 11beta-HSD1, which then exerts genomic effects via the glucocorticoid receptor. Chronic administration increases plasma glucocorticoid levels, body weight gain, and adiposity in mice, and induces insulin resistance. It also dose-dependently inhibits aldosterone.
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| ln Vivo |
Chronic administration of 11-dehydrocorticosterone to mice increases plasma glucocorticoid levels, body weight gain, and adiposity, and induces insulin resistance. In cardiac fibroblasts, it increases SGK mRNA expression. These in vivo effects are mediated through its conversion to active corticosterone by 11beta-HSD1. The compound has also been studied in animal models of stress and metabolic disease.
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| Enzyme Assay |
Not explicitly detailed in reference sources. However, an ELISA has been developed for the measurement of serum 11-dehydrocorticosterone in rats and mice. The antiserum against 11-dehydrocorticosterone allows specific detection without cross-reactivity with other corticosteroids. This immunoassay is used in preclinical studies to measure 11beta-HSD1 activity in murine models.
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| Cell Assay |
Not explicitly detailed in reference sources. For cell-based studies, cardiac fibroblasts are treated with 11-dehydrocorticosterone at various concentrations (0-1000 nM), and SGK mRNA expression is measured by quantitative PCR. The compound is typically dissolved in DMSO (≤0.1% final concentration) and diluted in serum-free medium before addition to cells.
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| Animal Protocol |
In mouse models of insulin resistance, 11-dehydrocorticosterone is administered chronically (e.g., via subcutaneous osmotic minipump or daily injection) at doses that achieve elevated plasma glucocorticoid levels. Body weight, food intake, glucose tolerance, and insulin sensitivity are measured. In some studies, 11-dehydrocorticosterone is used as a tool to manipulate local glucocorticoid availability.
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| ADME/Pharmacokinetics |
11-Dehydrocorticosterone has a molecular weight of 344.44 and formula C21H28O4. It is soluble in DMSO (20 mg/mL, 58.06 mM). Storage should be at -20degC as powder. The compound is a steroid hormone that is relatively stable when stored dry. For biological studies, it is typically dissolved in ethanol or DMSO and diluted in appropriate buffers or culture media.
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| Toxicity/Toxicokinetics |
Chronic administration of 11-dehydrocorticosterone to mice increases plasma glucocorticoid levels, body weight gain, and adiposity, and induces insulin resistance. While these effects are of pharmacological interest, they also represent potential toxicities (e.g., metabolic syndrome, hyperglycemia) that would be of concern for any drug candidate that elevates local glucocorticoid activity.
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| References | |
| Additional Infomation |
11-Dehydrocorticosterone is an 11-oxosteroid, a derivative of corticosterone, formed by the oxidation of the hydroxyl substituent at the 11β position to the corresponding ketone. It is a metabolite in both humans and mice. It is a 21-hydroxysteroid, 3-oxo-Δ⁴ steroid, 20-oxosteroid, 11-oxosteroid, corticosteroid, and primary α-hydroxy ketone. Functionally, it is related to corticosterone.
11-Dehydrocorticosterone is an endogenous metabolite of corticosterone and a research tool for studying glucocorticoid metabolism and 11beta-HSD1 activity. It has no approved clinical indications as a therapeutic agent. Measurement of 11-dehydrocorticosterone levels in biological samples (by LC-MS/MS or ELISA) can serve as a biomarker of 11beta-HSD1 activity in preclinical studies. |
| Molecular Formula |
C21H28O4
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|---|---|
| Molecular Weight |
344.44462
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| Exact Mass |
344.199
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| CAS # |
72-23-1
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| PubChem CID |
5311364
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| Appearance |
White to off-white solid powder
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| Density |
1.21g/cm3
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| Boiling Point |
530ºC at 760 mmHg
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| Flash Point |
288.4ºC
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| Index of Refraction |
1.567
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| LogP |
2.874
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
677
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2C(=O)C[C@]4([C@H]3CC[C@@H]4C(=O)CO)C
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| InChi Key |
FUFLCEKSBBHCMO-KJQYFISQSA-N
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| InChi Code |
InChI=1S/C21H28O4/c1-20-8-7-13(23)9-12(20)3-4-14-15-5-6-16(18(25)11-22)21(15,2)10-17(24)19(14)20/h9,14-16,19,22H,3-8,10-11H2,1-2H3/t14-,15-,16+,19+,20-,21-/m0/s1
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| Chemical Name |
(8S,9S,10R,13S,14S,17S)-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthrene-3,11-dione
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.9033 mL | 14.5163 mL | 29.0326 mL | |
| 5 mM | 0.5807 mL | 2.9033 mL | 5.8065 mL | |
| 10 mM | 0.2903 mL | 1.4516 mL | 2.9033 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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