| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Cortisol 21-sulfate is a steroid sulfate obtained by the formal condensation of hydroxy group at position 21 of cortisol with sulfuric acid.It has a role as a human metabolite. It is a steroid sulfate, an 11beta-hydroxy steroid, a 17alpha-hydroxy steroid, a 20-oxo steroid, a 3-oxo-Delta(4) steroid, a tertiary alpha-hydroxy ketone and a cortisol ester.
| Targets |
Intracellular transcortin (corticosteroid-binding globulin, CBG); glucocorticoid receptor (weak).
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| ln Vitro |
Cortisol 21-sulfate is a specific ligand for intracellular transcortin; it is a major metabolite of cortisol and has relatively low glucocorticoid activity compared to its parent compound cortisol, but it may modulate cortisol bioavailability and signaling; its levels in urine reflect adrenocortical activity.
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| ln Vivo |
Cortisol sulfate (3 mg; IM; every other day; for 2-7 weeks) impacts behavior through its direct effects on the central nervous system [4].
Not applicable (endogenous metabolite); as a naturally occurring metabolite, it is used as a biomarker rather than a therapeutic agent; its concentration in urine and plasma is used clinically to assess adrenocortical function, and abnormalities in its levels may indicate disorders such as Cushing‘s syndrome or adrenal insufficiency. |
| Enzyme Assay |
Binding to transcortin is assessed by radioligand binding assays using purified CBG (transcortin) and 3H-cortisol; increasing concentrations of non-labeled Cortisol 21-sulfate are added to displace radiolabeled cortisol; bound and free ligand are separated by charcoal adsorption or filtration, and radioactivity is measured by scintillation counting to determine IC50 or Ki.
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| Cell Assay |
Cellular activity assays are not typical for an endogenous metabolite; however, its effects on cortisol signaling can be assessed in glucocorticoid-responsive cell lines (e.g., hepatocytes or lymphocytes) by measuring glucocorticoid receptor (GR) transactivation; cells are treated with Cortisol 21-sulfate alone or in combination with cortisol; reporter gene assays (GRE-luciferase) or qPCR for GR target genes (e.g., GILZ, MKP-1) are performed.
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| Animal Protocol |
Animal/Disease Models: Male Wistar-King rat [4]
Doses: 3 mg Route of Administration: intramuscularinjection, every other day, for 2-7 weeks Experimental Results: The animal's exploratory behavior (walking and standing) was Dramatically improved during treatment The stimulating effect begins soon after weaning (21-24 days postpartum). Cortisol 21-sulfate is an endogenous compound; animal studies typically involve measuring its levels in urine or plasma under various physiological or pathological conditions (e.g., stress, adrenalectomy, glucocorticoid administration); no exogenous administration studies are typically performed. |
| ADME/Pharmacokinetics |
PK: Cortisol 21-sulfate is produced from cortisol by sulfotransferase enzymes (e.g., SULT2A1) in the adrenal cortex and liver; it circulates in plasma bound to transcortin and albumin; it is eliminated primarily in urine; its half-life is longer than that of free cortisol due to reduced hepatic clearance and increased protein binding.
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| Toxicity/Toxicokinetics |
Toxicity: Cortisol 21-sulfate is an endogenous metabolite and is generally considered non-toxic at physiological concentrations; very high concentrations (supraphysiological) have not been studied in toxicity models; the parent compound cortisol can cause toxicity at high doses (Cushing's syndrome), but the sulfated metabolite has much lower glucocorticoid activity.
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| References | |
| Additional Infomation |
Cortisol 21-sulfate is a steroidal sulfate formed by the condensation of the 21-hydroxyl group of cortisol with sulfuric acid. It is a human metabolite. It is a steroidal sulfate, 11β-hydroxysteroid, 17α-hydroxysteroid, 20-oxosteroid, 3-oxo-Δ⁴steroid, tertiary α-hydroxyketone, and cortisol ester. It is the conjugate acid of cortisol 21-sulfate (1-).
Cortisol 21-sulfate is an endogenous metabolite and analytical standard; it is not a drug and has no approval for therapeutic use; it is used in clinical chemistry as a urinary biomarker for adrenocortical function; in research, it serves as a reference compound for cortisol metabolism studies and for investigating corticosteroid transport and signaling; it is available as a reference standard for LC-MS/MS quantification in biological samples. |
| Molecular Formula |
C21H30O8S
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|---|---|
| Molecular Weight |
442.5231
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| Exact Mass |
442.166
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| CAS # |
1253-43-6
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| Related CAS # |
Cortisol sulfate sodium;1852-36-4
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| PubChem CID |
102172
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.689
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
905
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| Defined Atom Stereocenter Count |
7
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| SMILES |
OS(OCC(C1(CCC2C3CCC4=CC(CCC4(C)C3C(CC12C)O)=O)O)=O)(=O)=O
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| InChi Key |
JOVLCJDINAUYJW-VWUMJDOOSA-N
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| InChi Code |
InChI=1S/C21H30O8S/c1-19-7-5-13(22)9-12(19)3-4-14-15-6-8-21(25,17(24)11-29-30(26,27)28)20(15,2)10-16(23)18(14)19/h9,14-16,18,23,25H,3-8,10-11H2,1-2H3,(H,26,27,28)/t14-,15-,16-,18+,19-,20-,21-/m0/s1
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| Chemical Name |
[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] hydrogen sulfate
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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 | 2.2598 mL | 11.2989 mL | 22.5978 mL | |
| 5 mM | 0.4520 mL | 2.2598 mL | 4.5196 mL | |
| 10 mM | 0.2260 mL | 1.1299 mL | 2.2598 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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