DHEA (Synonyms: 脫氫表雄酮）
DHEA (Prasterone) 是最-豐富的類固醇激素之一。 DHEA通過(guò)多種信號(hào)傳導(dǎo)途徑介導(dǎo)其作用，并通過(guò)轉(zhuǎn)化成雄激素和雌激素衍生物（例如，雄激素，雌激素，7α和7β DHEA (Prasterone)，以及7α和7β表雄甾酮衍生物）通過(guò)其特異性受體起作用。
生物活性
DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors
IC50 & Target
Human Endogenous Metabolite
體外研究(In Vitro)
DHEA (Prasterone) is an effective antiapoptotic factor, reversing the serum deprivation-induced apoptosis in prostate cancer cells (DU145 and LNCaP cell lines) as well as in colon cancer cells (Caco2 cell line). DHEA (Prasterone) significantly reduces serum deprivation-induced apoptosis in all 3 cancer cell types, quantitated with the APOPercentage assay (apoptosis is reduced from 0.587±0.053 to 0.142±0.0016 or 0.059±0.002 after treatment for 12 hours with DHEA or NGF, respectively; n=3, P<0.01), and by flow cytometry analysis (FACS) for DU145 cells. The antiapoptotic effect of DHEA is dose dependent with an EC50 at nanomolar concentrations (EC50: 11.2±3.6 nM and 12.4±2.2 nM in DU145 and Caco2 cells, respectively)[1]. DHEA (Prasterone) is the principal sex steroid precursor in humans and can be converted directly to androgens. DHEA (Prasterone) (≥1 μM) causes a dose-dependent inhibition of Chub-S7 proliferation, as assessed by thymidine incorporation assays. DHEA (Prasterone) treatment inhibits expression of the key glucocorticoid-regulating genes H6PDH (≥100 nM) and HSD11B1 (≥1 μM) in differentiating preadipocytes in a dose-dependent manner. In keeping with this finding, DHEA (Prasterone) treatment (≥1 μM) results in a marked reduction in 11β-HSD1 oxoreductase activity (≥1 μM) and a concurrent increase in dehydrogenase activity at the highest DHEA dose used (25 μM DHEA) in differentiated adipocytes[2].
體內(nèi)研究(In Vivo)
DHEA (Prasterone) in the diet (0.45 % w/w) of male B6 mice (groups of five mice) treated for 8 weeks led to significant decreases in body temperature compared with mice fed the control AIN-76A diet. A similar comparison indicated that control and pair-fed mice are also significantly different. Animals fed DHEA (Prasterone) have significantly lower temperatures than mice fed the control diet 26/29 times tested; mice pair fed to those on the DHEA (Prasterone) diet are less affected, with 8/29 values significantly lower than in mice fed AIN-76A ad libitum. The temperatures of mice fed DHEA (Prasterone) or pair fed to DHEA (Prasterone) are significantly different 21/29 times tested. Body weights are significantly greater in mice fed the control diet than in mice fed DHEA or pair fed to DHEA (Prasterone). Food intake (grams per day) from cages are averaged for each week (n=7), except for Week 9 (n=3). The amount of food intake is significantly decreased in mice fed DHEA (Prasterone). By design, mice pair fed to DHEA (Prasterone) ate about the same amount. Thus, it appears that DHEA (Prasterone) reduces body temperature by food restriction and by a separate mechanism[3].
分子量：288.42
Formula：C19H28O2
CAS 號(hào)：53-43-0
中文名稱：脫氫表雄酮；去氫表雄酮；脫氫表雄甾酮；脫氫異雄酮；反式-脫氫異雄甾酮；反式-脫氫雄甾酮；脫氫表雄至素酮
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式：
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
Ethanol : 50 mg/mL (173.36 mM; Need ultrasonic)
DMSO : 50 mg/mL (173.36 mM; Need ultrasonic)
H2O : 1 mg/mL (3.47 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.4672 mL | 17.3358 mL | 34.6717 mL |
| 5 mM | 0.6934 mL | 3.4672 mL | 6.9343 mL |
| 10 mM | 0.3467 mL | 1.7336 mL | 3.4672 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶
- 1.
請(qǐng)依序添加每種溶劑： Cremophor EL
Solubility: 14.29 mg/mL (49.55 mM); Clear solution; Need ultrasonic
- 2.
請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution
- 3.
請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution
- 4.
請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution
- 5.
請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution
- 6.
請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (4.33 mM); Clear solution
- 7.
請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (4.33 mM); Clear solution
參考文獻(xiàn)
[1]. Anagnostopoulou V, et al. Differential effects of dehydroepiandrosterone and testosterone in prostate and colon cancer cell apoptosis: the role of nerve growth factor (NGF) receptors. Endocrinology. 2013 Jul;154(7):2446-56.
[2]. McNelis JC, et al. Dehydroepiandrosterone exerts anti-glucocorticoid action on human preadipocyte proliferation, differentiation and glucose uptake. Am J Physiol Endocrinol Metab. 2013 Nov 1;305(9):E1134-44.
[3]. Catalina F, et al. Decrease of core body temperature in mice by dehydroepiandrosterone. Exp Biol Med (Maywood). 2002 Jun;227(6):382-8.
注：產(chǎn)品僅用于科研
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