| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Mineralocorticoid Receptor (agonist). Endogenous metabolite produced by CYP11B2.
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|---|---|
| ln Vitro |
18-Oxocortisol is a naturally occurring mineralocorticoid agonist. Its receptor binding and activation properties have been characterized, demonstrating typical mineralocorticoid activity. Specific IC50 values for non-cell receptor binding are not detailed in standard references; functional assays confirm agonist activity.
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| ln Vivo |
Rats given 18-oxycortisol are shown to develop mineralocorticoid hypertension, which is linked to hypokalemia, cardiac and renal hypertrophy, and cardiovascular disease. A sharp rise in blood pressure was also observed in lambs given an injection of 18-oxycortisol. Raising blood pressure, however, requires substantial amounts [3]. In comparison with control rats, SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly slowed tumor growth (reduction of >50% on day 18) [1].
Administration of 18-oxocortisol to rats induces mineralocorticoid-type hypertension with hypokalemia, cardiac and renal enlargement, and cardiovascular lesions. In sheep, it causes a rapid increase in blood pressure, though relatively high doses are required for pressor effects. |
| Enzyme Assay |
Mineralocorticoid receptor (MR) binding assay: Competitive displacement of [3H]-aldosterone from recombinant human MR in cell-free buffer system. Compound incubated with MR and radioligand; bound vs free separated by filtration or charcoal; IC50/Ki calculated from concentration-response curves.
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| Cell Assay |
Not typically used in cell-based assays; as a biomarker and mineralocorticoid agonist, its activity is evaluated in functional assays (e.g., reporter gene assays in HEK293 cells expressing MR, measuring luciferase activity after 18-oxocortisol treatment). Specific protocols not detailed in standard references.
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| Animal Protocol |
Rat hypertension model: Male rats (strain not specified) administered 18-oxocortisol (dose not specified; likely mg/kg range) via subcutaneous injection or oral gavage. Blood pressure monitored via tail-cuff or telemetry; electrolyte levels, organ weights (heart, kidney), and histopathology assessed after chronic treatment.
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| ADME/Pharmacokinetics |
PK data for 18-oxocortisol not detailed in standard references; as an endogenous steroid, it undergoes typical corticosteroid metabolism (hepatic reduction and conjugation). It is detectable in plasma and urine as a biomarker. Clinical PK studies in humans are limited.
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| Toxicity/Toxicokinetics |
Administration of 18-oxocortisol to rats induces mineralocorticoid-type hypertension and hypokalemia, cardiac enlargement, and cardiovascular lesions. Thymus involution is observed, consistent with glucocorticoid activity. The compound has both mineralocorticoid and glucocorticoid properties, contributing to its toxicity profile.
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| References | |
| Additional Infomation |
18-Oxocortisol is a naturally occurring mineralocorticoid agonist and adrenal biomarker produced by CYP11B2. It is used in adrenal vein sampling as a biomarker for subclassifying primary aldosteronism. Not a therapeutic drug; serves as a diagnostic tool and research probe for steroidogenesis and adrenal pathophysiology.
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| Molecular Formula |
C₂₁H₂₈O₆
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|---|---|
| Molecular Weight |
376.44
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| Exact Mass |
376.189
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| CAS # |
2410-60-8
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| PubChem CID |
123712
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| Appearance |
White to off-white solid powder
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| LogP |
0.96
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
728
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2[C@H](C[C@]4([C@H]3CC[C@@]4(C(=O)CO)O)C=O)O
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| InChi Key |
XUQWWIFROYJHCU-UKSDXMLSSA-N
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| InChi Code |
InChI=1S/C21H28O6/c1-19-6-4-13(24)8-12(19)2-3-14-15-5-7-21(27,17(26)10-22)20(15,11-23)9-16(25)18(14)19/h8,11,14-16,18,22,25,27H,2-7,9-10H2,1H3/t14-,15-,16-,18+,19-,20+,21-/m0/s1
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| Chemical Name |
(8S,9S,10R,11S,13R,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-10-methyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-13-carbaldehyde
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| Synonyms |
18Oxocortisol; 18 Oxocortisol
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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 | 2.6565 mL | 13.2823 mL | 26.5647 mL | |
| 5 mM | 0.5313 mL | 2.6565 mL | 5.3129 mL | |
| 10 mM | 0.2656 mL | 1.3282 mL | 2.6565 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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