Testosterone undecanoate
(Synonyms: 十一酸睾酮,Testosterone undecylate) 目录号 : GC63217
Testosterone undecanoate是一种口服的合成代谢类固醇睾酮的酯前体药，可作为一种有效的睾酮替代疗法。
Cas No.:5949-44-0
Sample solution is provided at 25 µL, 10mM.
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Testosterone undecanoate, an orally administered ester prodrug of the anabolic steroid of testosterone, acts as an effective testosterone replacement therapy[1]. Testosterone undecanoate demonstrates the capability to stabilize testosterone levels while creating azoospermia conditions in men[2]. Testosterone undecanoate serves as a treatment for hypogonadism and is being tested for male contraceptive use[2].
In vitro, Testosterone undecanoate has anti-proliferative activity[3]. Treatment of 200μg/ml testosterone undecanoate plus 0.1μg/ml anastrozole for 24-48 hours can inhibit the proliferation of MCF-7 cells, promote cell apoptosis, and cause a significant decrease in androgen receptor protein expression[3].
In vivo, Testosterone undecanoate can cause benign prostatic hyperplasia[4]. Subcutaneous injection of 125mg/kg Testosterone undecanoate every 2-3 weeks caused high serum levels of testosterone, dihydrotestosterone, and 5-alpha reductase in castrated male Wistar rats (12 week-age), accompanied by elevated prostate weight, prostate volume, and prostate index[4]. Intramuscular injection of 1000mg Testosterone undecanoate at 12-week intervals was well tolerated in male hypogonadism patients, resulting in a return of testosterone levels to the normal range (16.5±8.0nmol/L)[5]. Following intramuscular injection of Testosterone undecanoate (20mg/kg/week) in male adult rhesus monkeys for 60 days, massive germ cell apoptosis occurred in the testis, and the HSP70-2 mRNA and protein levels decreased significantly[6-7]. Intramuscular injection of Testosterone undecanoate (500mg/kg/45days) caused the improved locomotor activity, the enhanced preference to novel objects, spatial memory, and reversed anxiety and depression induced by AlCl3+D-galactose administration in male mice with Alzheimer's disease, along with the altered gene expression levels of Na/K ATPase isoforms in the hippocampus of the brain[8].
References:
[1]Zgair A, Dawood Y, Ibrahem S M, et al. Predicting intestinal and hepatic first-pass metabolism of orally administered testosterone undecanoate[J]. Applied Sciences, 2020, 10(20): 7283.
[2]Yu M, Cao X, Xu J, et al. Effects of testosterone undecanoate as a male contraceptive candidate on rat immunological features[J]. Immunopharmacology and immunotoxicology, 2003, 25(4): 627-643.
[3] Chen R, Cui J, Wang Q, et al. Antiproliferative effects of anastrozole on MCF‑7 human breast cancer cells in vitro are significantly enhanced by combined treatment with testosterone undecanoate[J]. Molecular Medicine Reports, 2015, 12(1): 769-775.
[4]An J, Kong H. Comparative application of testosterone undecanoate and/or testosterone propionate in induction of benign prostatic hyperplasia in Wistar rats[J]. PloS one, 2022, 17(5): e0268695.
[5]Schubert M, Minnemann T, Hubler D, et al. Intramuscular testosterone undecanoate: pharmacokinetic aspects of a novel testosterone formulation during long-term treatment of men with hypogonadism[J]. The Journal of Clinical Endocrinology & Metabolism, 2004, 89(11): 5429-5434.
[6]Zhou X C, Zhang Z H, Hu Z Y, et al. Expression of Hsp70–2 in rhesus monkey testis during germ cell apoptosis induced by testosterone undecanoate[J]. Contraception, 2002, 66(5): 377-382.
[7]Zhang Z H, Zhou X C, Wei P, et al. Expression of Bcl-2 and Bax in rhesus monkey testis during germ cell apoptosis induced by testosterone undecanoate[J]. Archives of andrology, 2003, 49(6): 439-447.
[8]Elfouly A, Awny M, Ibrahim M K, et al. Effects of Long-Acting Testosterone Undecanoate on Behavioral Parameters and Na+, K+-ATPase mRNA Expression in Mice with Alzheimers Disease[J]. Neurochemical Research, 2021, 46(9): 2238-2248.
Testosterone undecanoate是一种口服的合成代谢类固醇睾酮的酯前体药，可作为一种有效的睾酮替代疗法[1]。Testosterone undecanoate具有在造成男性无精子症的情况下稳定睾酮水平的能力[2]。Testosterone undecanoate被用作治疗性腺功能减退症，并被测试用于男性避孕[2]。
Testosterone undecanoate在体外具有抗增殖活性[3]。200μg/ml的Testosterone undecanoate联合0.1μg/ml阿那曲唑处理MCF-7细胞24-48h可抑制细胞增殖，促进细胞凋亡，并引起雄激素受体蛋白表达明显下降[3]。
Testosterone undecanoate在体内可引起良性前列腺增生[4]。12周龄雄性Wistar大鼠去势后，每2-3周皮下注射125mg/kg的Testosterone undecanoate，导致血清睾酮、双氢睾酮和5-α还原酶水平升高，并伴有前列腺重量、前列腺体积和前列腺指数升高[4]。男性性腺功能减退症患者每隔12周肌内注射1000mg的Testosterone undecanoate可使睾酮水平恢复至正常范围（16.5±8.0nmol/L）[5]。成年雄性恒河猴肌内注射Testosterone undecanoate（20mg/kg/周）60天后，睾丸出现大量生殖细胞凋亡，HSP70-2 的mRNA和蛋白水平显著下降[6-7]。肌内注射Testosterone undecanoate（500mg/kg/45天）改善了阿尔茨海默病雄性小鼠的自主活动，增强了对新事物的偏好和空间记忆，并逆转了由AlCl3+D-半乳糖诱导的焦虑和抑郁症状，同时改变了大脑海马Na/K ATP酶各异型基因的表达水平[8]。
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation Method | Approximately 5×104 MCF-7 cells were distributed into 6-well plates with 2 ml Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), and 5×103 MCF-7 cells were placed into 96-well plates using 0.2 ml DMEM with 10% FBS. The cells grew in an atmosphere enriched with 5% CO2 at a temperature of 37°C. During the experiment the cell density reached between 60 and 70% confluency at which point the existing media was changed. The stock solutions of anastrozole and testosterone undecanoate underwent dilution in DMEM with 5% FBS before application. Cells were treated with 0.1 or 0.01μg/ml anastrozole. The combinations of anastrozole and testosterone undecanoate used for the in vitro investigations were: 0.1μg/ml anastrozole with either 20 or 200μg/ml Testosterone undecanoate and 0.01μg/ml anastrozole with either 20 or 200μg/ml Testosterone undecanoate. After applying testosterone undecanoate for time intervals of 24, 48 and 72 hours the cells from the 6-well plate were collected for western blotting and flow cytometric analysis while cells from the 96-well plate were collected for the CCK-8 assay. |
Reaction Conditions | 20 or 200μg/ml; 0, 24, 48 and 72 hours |
Applications | Testosterone undecanoate and anastrozole have antiproliferative activity, causing the high percentage of apoptotic cells and significant decrease in androgen receptor protein expression. |
| Animal experiment [2]: | |
Animal models | Male New Zealand white rabbits |
Preparation Method | 24 male New Zealand white rabbits who weighed an average of 2500g at three months old were employed. Each rabbit was kept alone under a 12-hour light schedule with room temperature maintained at 20°C. During 18-week period the rabbits received unrestricted access to a commercial rabbit food. Split the rabbits into three groups (Group 1-3) with each group containing 8 rabbits. Group 1 acts as the control group without any alterations. Anesthetize rabbits in Groups 2 and 3 with ketamine (35mg/kg) and xylazine (5mg/kg) before performing bilateral castration through 3-cm scrotal incisions. The Group 3 received an initial intramuscular injection of Testosterone undecanoate (6mg/kg) in the gluteal region followed by another injection after 6 weeks. Measurements of whole blood viscosity and various biochemical parameters including total plasma testosterone, hemoglobin (Hb), hematocrit (Hct), fibrinogen (FBN), total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C) were conducted at baseline as well as at 6-week and 18-week intervals. |
Dosage form | 6mg/kg/dosage; 1, 6 and 18 weeks; i.m. |
Applications | Testosterone undecanoate treatment reduces whole blood viscosity and increases fibrinogen, hemoglobin and hematocrit levels during 6 weeks. |
References: | |
| Cas No. | 5949-44-0 | SDF | |
| 别名 | 十一酸睾酮,Testosterone undecylate | ||
| 分子式 | C30H48O3 | 分子量 | 456.7 |
| 溶解度 | DMSO : 10 mg/mL (21.90 mM; Need ultrasonic and warming) | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1896 mL | 10.9481 mL | 21.8962 mL |
| 5 mM | 0.4379 mL | 2.1896 mL | 4.3792 mL |
| 10 mM | 0.219 mL | 1.0948 mL | 2.1896 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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。
1. 首先保证母液是澄清的；
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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