5β-Androstan-3β-ol-17-one (3β-Etiocholanolone; 5β-Epiandrosterone)   中文名称: 5b-雄甾3b-醇-17-酮

Endogenous metabolite

表胆甾醇酮是一种3 -羟基类固醇，由5 -雄甾烷在3 -位置被羟基取代，在17号位置被氧基取代。它是睾酮的代谢物。它具有雄激素、人血清代谢物、小鼠代谢物、大鼠代谢物和动物代谢物的作用。它是一种3 -羟基类固醇，一种17-氧类固醇和一种雄激素。它来源于5 -雄甾烷的氢化物。

5β-Androstan-3β-ol-17-one（2 mg/小鼠；皮下注射；每天一次，持续 4 周）无效意味着这些代谢物需要进行一些生物转化才能正常发挥作用[1]。添加到食物中的 5β-Androstan-3β-ol-17-one（口服治疗；总共 18 周；质量比分别为 0.025%、0.05% 和 0.1%）可预防小鼠患严重糖尿病并控制高血糖。正常化而不影响食物消耗或体重增加率[1]。单剂量静脉注射时，5β-Androstan-3β-ol-17-one (1 mg/kg–20 mg/kg) 对成年雄性猫神经元表现出有效的抑制作用[2]。

Animal/Disease Models: C57BL/KsJ genetically diabetic (db/db) mice model[1]
Doses: 0.025%, 0.05%, 0.1% in diet
Route of Administration: Oral gavage; filled the diet every second day; for 18 weeks
Experimental Results: Exerted strong antihyperglycemic effects.

[1]. Coleman DL, et al. Therapeutic effects of dehydroepiandrosterone metabolites in diabetes mutant mice (C57BL/KsJ-db/db). Endocrinology. 1984 Jul;115(1):239-43.
[2]. Kubli-Garfias C, et al. Depressant effect of androgens on the cat brain electrical activity and its antagonism by ruthenium red. Neuroscience. 1982;7(11):2777-82.

Epietiocholanolone is a 3beta-hydroxy steroid that is 5beta-androstane substituted by a hydroxy group at position 3beta and an oxo group at position 17. It is a metabolite of testosterone. It has a role as an androgen, a human blood serum metabolite, a mouse metabolite, a rat metabolite and an animal metabolite. It is a 3beta-hydroxy steroid, a 17-oxo steroid and an androstanoid. It derives from a hydride of a 5beta-androstane.

---

Dehydroepiandrosterone (DHEA) fed at 0.4% in the diet is known to exert strong antihyperglycemic effects in C57BL/KsJ genetically diabetic (db/db) mice. Three of the major metabolic products of DHEA; DHEA sulfate, alpha-hydroxyetiocholanolone (alpha-ET), and beta-hydroxyetiocholanolone (beta-ET) when fed at 0.1% in the diet, and one putative product, 17 beta-estradiol, when fed at 0.005% also prevented the development of severe diabetes while having little effect on the amount of food eaten or the rate of weight gain. When suboptimal doses (5-20 micrograms/week) of estradiol were injected in combination with diets containing either alpha-ET or beta-ET, marked potentiating effect was noted, normalization of the hyperglycemia being produced with as little as 0.025% of beta-ET and 0.05% of alpha-ET. The ability of the etiocholanolones to maintain islet integrity and prevent the development of most diabetes symptoms suggests that these metabolites are not merely inactive end products of steroid metabolism, but are physiological effectors in their own right.[1]

---

Electroencephalographic synchronization and a fall in the multiunit activity was observed in the mesencephalic reticular formation, ventromedial hypothalamus and dorsal hippocampus following intravenous administration of some 5 alpha and 5 beta-reduced testosterone derivatives. The most potent compounds were androsterone and androstanediol which have the 3 alpha-hydroxy-5 alpha ring A configuration. Steroids with 5 beta reduction, i.e. 5 beta-dihydrotestosterone, etiocholanolone and epi-etiocholanolone, at high doses produced the inhibitory effect. Testosterone and its closer 5 alpha metabolites (5 alpha-dihydrotestosterone and 5 alpha-androstanedione) were ineffective. The depressive effect of androsterone on neurones was antagonized by the intraventricular injection of ruthenium red. On the other hand, the convulsant effect of ruthenium red was prevented or diminished by the action of androsterone. These findings support the hypothesis that testosterone metabolites reduced either at 5 alpha or 5 beta position can act in the brain at a membrane level and raise the possibility that testosterone may be a prehormone in the regulation of excitability in some brain functions.[2]

C19H30O2

290.44

290.225

571-31-3

247732

Typically exists as solid at room temperature

1.085 g/cm3

413.1ºC at 760 mmHg

154-156ºC

176.4ºC

1.536

3.959

37.3

1

2

0

21

459

7

CC12CCC(CC1CCC3C2CCC4(C3CCC4=O)C)O

QGXBDMJGAMFCBF-XRJZGPCZSA-N

InChI=1S/C19H30O2/c1-18-9-7-13(20)11-12(18)3-4-14-15-5-6-17(21)19(15,2)10-8-16(14)18/h12-16,20H,3-11H2,1-2H3/t12-,13+,14+,15+,16+,18+,19+/m1/s1

(3S,5R,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

Epietiocholanolone; 571-31-3; 5beta-androstan-3beta-ol-17-one; 3beta-hydroxy-5beta-androstan-17-one; 5b-Epiandrosterone; beta-Etiocholanolone; 3b-hydroxy-5b-androstan-17-one; 3.beta.-Etiocholanolone;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

---

注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

View More

注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

---

口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

View More

口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

---

注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。