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Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
For research use only. We do not sell to patients.
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality[1][2][3][4].
IC50 & Target
Human Endogenous Metabolite
Sigma 1 Receptor
PPARα
Cellular Effect
Cell Line
Type
Value
Description
References
CHO
EC50
127 μM
Compound: 50
Agonist activity at human TGR5 expressed in CHO cells by luciferase assay
Agonist activity at human TGR5 expressed in CHO cells by luciferase assay
Dehydroepiandrosterone sulfate (0.1 nM-10 μM; 2-24 h) increases neuronal survival in embryonic rat cortical cell hypoxia assay, with significant effects at 10 μM[1]. Dehydroepiandrosterone sulfate (0.1-10 μM) protects neurons in rat cerebellar granule cell oxygen-glucose deprivation assay in a dose-dependent manner, with almost complete protection at 10 μM[1]. Dehydroepiandrosterone sulfate (DHEAS) (1 μM-1 mM; 48 h) inhibits TNF-α-induced VCAM-1, IL-8, and ICAM-1 expression in human aortic endothelial cell inflammation assay, and inhibits NF-κB activity via activation of PPARα[5]. Dehydroepiandrosterone sulfate (DHEAS) (10-7-10-5 M; 96 h) inhibits LIF-induced proliferation of juvenile bovine chromaffin cells and enhances EGF-induced proliferation of adult bovine chromaffin cells in a proliferation assay[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Did not affect basal proliferation but inhibited LIF-induced proliferation by 30% at 10-5 M. In adult cells, enhanced EGF-induced proliferation by 25% at 10-5 M, without effect at lower concentrations.
In Vivo
Dehydroepiandrosterone sulfate (DHEAS) (1 mg/kg; intravenous injection; single dose) reduces the threshold shift of compound action potentials and the amplitude of distortion product otoacoustic emissions in the noise-induced cochlear injury model of albino guinea pigs, and has a protective effect on the cochlea[7]. Dehydroepiandrosterone sulfate (DHEAS) (converted from 2 mg/kg Dehydroepiandrosterone intraperitoneally; once daily; 13 days) can shorten the immobility time in the forced swim test in the male FSL rat model of depression, but when used in combination with electroconvulsive shock (ECS), it offsets the antidepressant effect of ECS[8].
Dehydroepiandrosterone sulfate (DHEAS) (10 mg/kg; subcutaneous injection; once daily; 4 weeks) enhances the seizure sensitivity of Laka mice in the pentylenetetrazol-induced seizure model, as shown by a decrease in the half effective dose of seizure (ED50 from 67.6 mg/kg to 48.6 mg/kg) and a shortens seizure latency, an effect that is reversed by Progesterone (HY-N0437) or Dizocilpine (HY-15084B)[9]. Chronic treatment with Dehydroepiandrosterone sulfate for 4 weeks significantly reduces the body weight of mice in the pentylenetetrazol-induced seizure model[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Albino Guinea Pig Noise-Induced Cochlear Injury Model (250-350 g): 2 kHz pure tone (120-125 dB SPL for 10 min) induced cochlear injury[7]
Dosage:
1 mg/kg Dehydroepiandrosterone sulfate
Administration:
Intravenous injection, single dose immediately before acoustic overexposure
Result:
Significantly improved cochlear function 1 week after acoustic exposure, reducing CAP threshold shifts and increasing DPOAE amplitude compared to control groups. The protective effect was observed at 1 mg/kg but not at 0.1 mg/kg, with no significant effect immediately after exposure.
Animal Model:
Flinder Sensitive Line (FSL) Rat Model of Depression (male, 200-220 g, 6-8 weeks old): forced swim test (FST) assay[8]
Dosage:
2 mg/kg Dehydroepiandrosterone (converted to Dehydroepiandrosterone sulfate)
Administration:
Intraperitoneal injection, daily for 13 days
Result:
Chronic Dehydroepiandrosterone administration (converted to Dehydroepiandrosterone sulfate) alone reduced immobility time in FST, mimicking antidepressant effects. Combined treatment with electroconvulsive shock (ECS) abolished this effect, with immobility time significantly increased compared to DHEA or ECS alone, indicating DHEAS may antagonize ECS efficacy.
Animal Model:
Mouse Pentylenetetrazol-Induced Seizure Model (20-25 g): Pentylenetetrazol-induced tonic convulsions[9]
Dosage:
10 mg/kg Dehydroepiandrosterone sulfate (dissolved in 0.1% Tween 80 saline)
Administration:
Subcutaneous injection, daily for 4 weeks
Result:
Chronic treatment shifted pentylenetetrazol dose-response curves leftward, reducing ED50 for convulsions and shortening latency to seizure onset, indicating enhanced seizure sensitivity.
This proconvulsant effect was prevented by co-treatment with progesterone or dizocilpine, linking it to GABAA receptor antagonism and NMDA receptor activation.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (271.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.7138 mL
13.5689 mL
27.1378 mL
5 mM
0.5428 mL
2.7138 mL
5.4276 mL
10 mM
0.2714 mL
1.3569 mL
2.7138 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.7138 mL
13.5689 mL
27.1378 mL
67.8444 mL
5 mM
0.5428 mL
2.7138 mL
5.4276 mL
13.5689 mL
10 mM
0.2714 mL
1.3569 mL
2.7138 mL
6.7844 mL
15 mM
0.1809 mL
0.9046 mL
1.8092 mL
4.5230 mL
20 mM
0.1357 mL
0.6784 mL
1.3569 mL
3.3922 mL
25 mM
0.1086 mL
0.5428 mL
1.0855 mL
2.7138 mL
30 mM
0.0905 mL
0.4523 mL
0.9046 mL
2.2615 mL
40 mM
0.0678 mL
0.3392 mL
0.6784 mL
1.6961 mL
50 mM
0.0543 mL
0.2714 mL
0.5428 mL
1.3569 mL
60 mM
0.0452 mL
0.2261 mL
0.4523 mL
1.1307 mL
80 mM
0.0339 mL
0.1696 mL
0.3392 mL
0.8481 mL
100 mM
0.0271 mL
0.1357 mL
0.2714 mL
0.6784 mL
Dehydroepiandrosterone sulfate Related Classifications
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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