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  3. Dehydroepiandrosterone sulfate

Dehydroepiandrosterone sulfate  (Synonyms: DHEA sulfate; Prasterone sulfate)

目录号: HY-113416 纯度: 99.93%
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Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) 是一种神经甾体和肾上腺的主要分泌产物。Dehydroepiandrosterone sulfate 同时具有 GABAA 受体的非竞争性拮抗剂和 σ1 受体的激动剂活性。Dehydroepiandrosterone sulfate 可部分透过血脑屏障,抑制 GABAA 受体介导的氯离子内流、通过 σ1 受体增强 NMDA 受体活性,发挥抗炎、抗糖皮质激素和抗抑郁的作用,并增加惊厥敏感性。Dehydroepiandrosterone sulfate 参与神经保护、神经突生长调控及儿茶酚胺分泌调节,可用于抑郁症、创伤后应激障碍 (PTSD)、阿尔茨海默病等研究。Dehydroepiandrosterone sulfate 也可能是心血管疾病死亡率的生物标志物,其浓度与死亡率呈独立且负相关的关系。

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Dehydroepiandrosterone sulfate

Dehydroepiandrosterone sulfate Chemical Structure

CAS No. : 651-48-9

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Other Forms of Dehydroepiandrosterone sulfate:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

细胞效力
(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
[PMID: 18307294]
体外研究
(In Vitro)

Dehydroepiandrosterone sulfate (0.1 nM-10 μM;2-24 h) 在胚胎大鼠皮层细胞缺氧实验中显示可提高神经元存活率,且 10 μM 时效果显著[1]
Dehydroepiandrosterone sulfate (0.1-10 μM) 在大鼠小脑颗粒细胞氧葡萄糖剥夺实验中呈剂量依赖性保护神经元,10 μM 时几乎完全保护[1]
Dehydroepiandrosterone sulfate (DHEAS) (1 μM-1 mM;48 h) 在人主动脉内皮细胞炎症实验中抑制 TNF-α 诱导的 VCAM-1、IL-8 和 ICAM-1 表达,并通过激活 PPARα 抑制 NF-κB 活性[5]
Dehydroepiandrosterone sulfate (DHEAS) (10-7-10-5 M;96 h) 在牛嗜铬细胞增殖实验中抑制幼年细胞的 LIF 诱导增殖,增强成年细胞的 EGF 诱导增殖[6]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human aortic endothelial cells (HAECs)
Concentration: 0.1 μM-1 mM
Incubation Time: 48 hours
Result: Had no significant effect on cell viability, as over 95% of cells remained viable across all concentrations tested, comparable to vehicle control.

RT-PCR[5]

Cell Line: Human aortic endothelial cells (HAECs)
Concentration: 1 mM
Incubation Time: 48 hours (pretreatment) + 4 hours (TNF-α stimulation)
Result: Significantly reduced TNF-α-induced IL-8 and ICAM-1 mRNA expression by 5-fold and 2-fold, respectively, compared to TNF-α alone.

Western Blot Analysis[5]

Cell Line: Human aortic endothelial cells (HAECs)
Concentration: 1-1000 μM
Incubation Time: 48 hours
Result: Increased IκB-α protein levels in a dose-dependent manner, with maximal induction at 1000 μM, correlating with NF-κB inhibition.

Cell Proliferation Assay[6]

Cell Line: Juvenile/adult bovine chromaffin cells
Concentration: 10-7-10-5 M
Incubation Time: 96 hours
Result: 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.
体内研究
(In Vivo)

Dehydroepiandrosterone sulfate (DHEAS) (1 mg/kg;静脉注射;单次) 降低白化豚鼠噪声性耳蜗损伤模型的复合动作电位阈值偏移,减少畸变产物耳声发射振幅,对耳蜗具有保护作用[7]
Dehydroepiandrosterone sulfate (DHEAS) (由 2 mg/kg Dehydroepiandrosterone 腹腔注射转化生成;每日 1 次;13 天) 可缩短雄性 FSL 大鼠的抑郁症模型在强迫游泳实验中的不动时间,但与电惊厥休克 (ECS) 联合使用时抵消 ECS 的抗抑郁效果[8]
Dehydroepiandrosterone sulfate (DHEAS) (10 mg/kg;皮下注射;每日 1 次;4 周) 增强 Laka 品系小鼠的 Pentylenetetrazol 诱导惊厥模型的惊厥敏感性,表现为降低惊厥半数有效剂量 (ED50 从 67.6 mg/kg 变为 48.6 mg/kg) 和缩短发作潜伏期,该效应可被 Progesterone (HY-N0437) 或 Dizocilpine (HY-15084B) 逆转[9]
Dehydroepiandrosterone sulfate 在 Pentylenetetrazol 诱发小鼠惊厥模型中慢性处理 4 周后小鼠体重显著下降[9]

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.
分子量

368.49

Formula

C19H28O5S

CAS 号
性状

固体

颜色

White to off-white

初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (271.38 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.78 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.78 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.93%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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