Androsterone (5α-Androstan-3α-ol-17-one)
(Synonyms: 雄酮; 5α-Androstan-3α-ol-17-one) 目录号 : GC30842
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Androsterone (5α-Androstan-3α-ol-17-one)是睾酮的一种代谢产物，可调节癫痫发作的易感性。
Cas No.:53-41-8
Sample solution is provided at 25 µL, 10mM.
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Androsterone (5α-Androstan-3α-ol-17-one) is a metabolite of testosterone that modulates the susceptibility of an epilepsy seizure [1]. Androsterone can alleviate the damaging effects of chilling stress by improving antioxidative system and enhancing carotenoid levels in maize seedlings [2]. Androsterone has been widely used to inhibit the proliferation of cardiac muscle cells and regulate the nuclear translocation of androgen receptors[3].
In vitro, Androsterone (75μM) treatment for 24 hours significantly reduced the viability of H9c2 cells, resulting in a decrease in the level of phosphorylated RB protein and inducing cell cycle arrest[4]. Treatment with 100μM Androsterone for 24 hours significantly induced the expression of small heterodimer partner (SHP) in AML-12 cells[5].
In vivo, Androsterone treatment via intraperitoneal injection at a dose of 200mg/kg/day for 2 days significantly increased the expression of Calbindin-D28k in the hippocampus of mice with status epilepticus (SE)[6]. A single intraperitoneal injection of 80mg/kg of Androsterone, lasting for 15 minutes, significantly increased the threshold for convulsions in mice[7].
References:
[1] Caliebe S V M, Pinacho P, Schnell M. Steroid hormone androsterone observed in the gas phase by rotational spectroscopy[J]. The Journal of Physical Chemistry Letters, 2022, 13(51): 11913-11917.
[2] Erdal S. Androsterone-induced molecular and physiological changes in maize seedlings in response to chilling stress[J]. Plant Physiology and Biochemistry, 2012, 57: 1-7.
[3] Androsterone has been widely used to inhibit the proliferation of cardiac muscle cells and regulate the nuclear translocation of androgen receptors.
[4] Huo Y, Wang W, Zhang J, et al. Maternal androgen excess inhibits fetal cardiomyocytes proliferation through RB-mediated cell cycle arrest and induces cardiac hypertrophy in adulthood[J]. Journal of endocrinological investigation, 2024, 47(3): 603-617.
[5] Wang S, Lai K D, Moy F J, et al. The nuclear hormone receptor farnesoid X receptor (FXR) is activated by androsterone[J]. Endocrinology, 2006, 147(9): 4025-4033.
[6] Cho I, Cho Y J, Kim H W, et al. Effect of androsterone after pilocarpine-induced status epilepticus in mice[J]. Journal of Epilepsy Research, 2014, 4(1): 7.
[7] Tutka P, Mróz K, Mróz T, et al. Effects of androsterone on the protective action of various antiepileptic drugs against maximal electroshock-induced seizures in mice[J]. Psychoneuroendocrinology, 2019, 101: 27-34.
Androsterone (5α-Androstan-3α-ol-17-one)是睾酮的一种代谢产物，可调节癫痫发作的易感性[1]。Androsterone可通过改善抗氧化系统和提高玉米幼苗中类胡萝卜素水平来减轻低温胁迫的损害效应[2]。Androsterone已被广泛用于抑制心肌细胞的增殖以及调节雄激素受体的核转位[3]。
在体外，75μM的Androsterone处理H9c2细胞24小时，显著降低了细胞活力，导致RB蛋白磷酸化水平下降并诱导细胞周期阻滞[4]。100μM的Androsterone处理AML-12细胞24小时，显著诱导了small heterodimer partner (SHP)的表达[4]。
在体内，每日腹腔注射200mg/kg剂量的Androsterone，连续2天，显著增加了癫痫持续状态小鼠海马中Calbindin-D28k的表达[6]。单次腹腔注射80mg/kg剂量的Androsterone，持续15分钟，显著提高了小鼠的惊厥阈值[7]。
| Cell experiment [1]: | |
Cell lines | H9c2 cells |
Preparation Method | H9c2 cells were incubated with high-glucose DMEM supplemented with 10% fetal bovine serum in a humidified atmosphere at 37°C with 5% CO2. H9c2 cells treated with different concentrations of Androsterone (0, 10, 50, 75, and 100μM) were seeded in 96-well culture plates (5000 cells/well) and incubated for 24h. Cell viability was measured. |
Reaction Conditions | 0, 10, 50, 75, and 100μM; 24h |
Applications | Androsterone treatment significantly reduced the cell viability of H9c2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male ICR mice |
Preparation Method | Male ICR mice were housed under a 12h light/dark cycle with food and water ad libitum. Lithium chloride (127mg/kg) was injected intraperitoneally (i.p.) 24h prior to pilocarpine administration. Next, mice were pretreated with methscopolamine-bromide (1mg/kg; i.p.) 30min prior to pilocarpine, and single dose of pilocarpine (30mg/kg; i.p.) was administered. Seizures were scored using Racine’s scale, and the duration of status epilepticus (SE) was determined by behavioral assessment. All mice received i.p. injections of 0.9% saline: 5ml twice on the day with SE and 5ml twice (in the morning and evening) of the day after SE. Two hours after SE, mice were treated with Androsterone (200mg/kg/day; i.p.). After 2 days, the brain tissues of the mice were removed for analysis. |
Dosage form | 200mg/kg/day for 2 days; i.p. |
Applications | Androsterone treatment significantly increased the expression of Calbindin-D28k in the hippocampus of mice with SE. |
References: | |
| Cas No. | 53-41-8 | SDF | |
| 别名 | 雄酮; 5α-Androstan-3α-ol-17-one | ||
| Canonical SMILES | C[C@]1([C@](CC2)([H])[C@]3([H])CC[C@@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC1)C2=O | ||
| 分子式 | C19H30O2 | 分子量 | 290.44 |
| 溶解度 | DMSO : 50 mg/mL (172.15 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at-20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4431 mL | 17.2153 mL | 34.4305 mL |
| 5 mM | 688.6 μL | 3.4431 mL | 6.8861 mL |
| 10 mM | 344.3 μL | 1.7215 mL | 3.4431 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >95.00% Appearance: A solid
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