Epiandrosterone
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50值：阻断心室肌细胞L-型钙通道，IC50值为42 ± 6 μM。
在外周组织形成的17-酮类固醇表雄酮(EPI)是睾酮前体脱氢表雄酮(DHEA)的代谢物。体内循环后，EPI最终从尿中排出。作为一种弱雄激素，经证实EPI可阻止磷酸戊糖途径(PPP)，且下调细胞内NADPH水平。最重要的是，EPI关闭心室肌细胞L-型钙通道且限制心肌收缩力[1]。
体外实验：经报道，10到100 mM浓度的EPI剂量依赖性地降低左心室发展压(LVDP)和心肌收缩率。此外，EPI也剂量依赖性地增加离体心脏内的CPP、下调心肌NADPH和亚硝酸盐的水平，以及松弛大鼠主动脉环。通过单心室肌细胞全细胞膜片钳的电生理分析，发现EPI可逆地和剂量依赖性地阻止由Ba2+载流的L-型通道电流，IC50值为42 ± 6 μM。此外，浓度为30 mM 的EPI加速去极化期间IBa的衰减，这表明该药剂作为L-型Ca2+通道拮抗剂，与1，4-二氢吡啶(DHP) Ca2+通道阻滞剂具有相似的特征[1]。
体内实验：使用G-6-PD低的C57L/J小鼠红细胞进行体内测试。连续七天给小鼠隔日口服450或900 mg/kg的检测试剂，包括DHEA、EPI、孕烯醇酮(PREG)及雄烯二酮(ANDR)。最后一次给药三小时后，处死小鼠。血液样本的调查结果表明，G-6-PD活性没有显著变化，这可能是由于红细胞膜上缺少类固醇受体位点引起的[2]。
临床试验：进行双盲临床试验，检测DHEA对自卑、信心不足及社交缺陷的八位精神病患者的作用。研究发现，在两项生产力测试中，DHEA对客观判断行为没有影响，也不具有调节性能[3]。
参考文献：
[1]Gupte SA, Tateyama M, Okada T, Oka M and Ochi R. Epiandrosterone, a metabolite of testosterone precursor, blocks l-type calcium channels of ventricular myocytes and inhibits myocardial contractility. J Mol Cell Cardiol. 2002 Mar; 34: 679- 88.
[2]Calabrese EJ, Horton HM and Leonard DA. The in vivo effects of four steroids on glucose-6-phosphate dehydrogenase activity of c57L/J mouse erythrocytes. J. Environ. Sci. Health. 1987; A22(6): 563-74.
[3]Forrest AD, Drewery J, Fotherby K and Laverty SG. A clinical trial of dehydroepiandrosterone (diandrone). J. Neurol. Neurosurg. Psychiat. 1960; 23: 52-5.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 290.44 |
| Cas No. | 481-29-8 |
| Formula | C19H30O2 |
| Solubility | insoluble in H2O; ≥12.35 mg/mL in EtOH; ≥28.27 mg/mL in DMSO |
| Chemical Name | (3S,5S,8R,9S,10S,13S,14S)-3-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,14,15,16-tetradecahydrocyclopenta[a]phenanthren-17-one |
| SDF | Download SDF |
| Canonical SMILES | O[C@@H]1C[C@H]2[C@@](CC1)(C)[C@@H]3[C@@H](CC2)[C@H](CCC4=O)[C@]4(C)CC3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
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Cell lines |
Ventricular myocytes |
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Reaction Conditions |
100 nM ~ 100 μM epiandrosterone |
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Applications |
Electrophysiological analysis of single ventricular myocytes using whole cell clamp showed epiandrosterone to dose-dependently (100 nM ~ 100 μM) and reversibly inhibit L-type channel currents carried by Ba2+ (IBa) (IC50 = 42 ± 6 μM) by as much as 50%. At 30 μM, epiandrosterone shifted the steady-state inactivation curve to more negative potentials, thereby accelerating the decay of IBa during depolarization. These results suggest that epiandrosterone may act as an L-type Ca2+ channel antagonist with properties similar to those of 1,4-dihydropyridine (DHP) Ca2+ channel blockers. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Gupte SA, Tateyama M, Okada T, et al. Epiandrosterone, a metabolite of testosterone precursor, blocks L-type calcium channels of ventricular myocytes and inhibits myocardial contractility. Journal of Molecular and Cellular Cardiology, 2002, 34(6): 679-688. |
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