Testosterone undecanoate
(Synonyms: 十一酸睾酮,Testosterone undecylate) 目录号 : GC63217
Testosterone undecanoate是睾酮酯，用做男性节育。
Cas No.:5949-44-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Testosterone undecanoate is an ester of testosterone; used in androgen replacement therapy primarily for the treatment of male hypogonadism, and is currently under research for use as a male contraceptive.
| 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。
Testosterone Undecanoate-Schering AG
Drugs R D 2004;5(6):368-9.PMID:15563244DOI:10.2165/00126839-200405060-00012.
Schering AG is developing a formulation of Testosterone undecanoate [Nebido] for the treatment of testosterone deficiency or hypogonadism. This deficiency can lead to decreased muscle mass, impaired muscle function, osteoporosis, reduced sexual function and mental degeneration. Schering claims that its new formulation provides superior control of blood levels of the drug and permits a longer period of application. Nebido requires only four injections per year, and represents a major improvement for men with testosterone deficiency. Schering AG received approval of its Testosterone undecanoate formulation in its first European country, Finland, in November 2003 for the treatment of hypogonadism in men. In July 2004, Schering's Testosterone undecanoate formulation completed approval of the European mutual recognition procedure. This approval clears the way for marketing the product (as Nebido) in the large pharmaceutical markets like Germany, France and the UK. The initial phase of the product launch will occur in Finland in October 2004, and in Germany in November 2004. Other European countries will follow in 2005, and following receipt of approval, it will be introduced in the first Latin American and Asian countries. In its 2002 Annual Report, Schering predicted that Testosterone undecanoate has the potential to reach peak sales of euro 100 million, 3 years after launch-launch in Europe was at the time anticipated in 2004.
A New Oral Testosterone undecanoate Formulation Restores Testosterone to Normal Concentrations in Hypogonadal Men
J Clin Endocrinol Metab 2020 Aug 1;105(8):2515-2531.PMID:32382745DOI:10.1210/clinem/dgaa238.
Context: A novel formulation of oral testosterone (T) undecanoate (TU) was evaluated in a phase 3 clinical trial. Objective: Determine efficacy, short-term safety, and alignment of new oral TU formulation with current US approval standards for T replacement therapy. Design: Randomized, active-controlled, open-label study. Setting and patients: Academic and private clinical practice sites; enrolled patients were clinically hypogonadal men 18 to 65 years old. Methods: Patients were randomized 3:1 to oral TU, as prescribed (JATENZO®; n = 166) or a topical T product once daily (Axiron®; n = 56) for 3 to 4 months. Dose titration was based on average T levels (Cavg) calculated from serial pharmacokinetic (PK) samples. T was assayed by liquid chromatography-mass spectrometry/mass spectrometry. Patients had 2 dose adjustment opportunities prior to final PK visit. Safety was assessed by standard clinical measures, including ambulatory blood pressure (BP). Results: 87% of patients in both groups achieved mean T Cavg in the eugonadal range. Sodium fluoride-ethylenediamine tetra-acetate plasma T Cavg (mean ± standard deviation) for the oral TU group was 403 ± 128 ng/dL (~14 ± 4 nmol/L); serum T equivalent, ~489 ± 155 ng/dL (17 ± 5 nmol/L); and topical T, 391 ± 140 ng/dL (~14 ± 5 nmol/L). Modeling/simulation of T PK data demonstrated that dose titration based on a single blood sample 4 to 6 h after oral TU dose yielded efficacy (93%) equivalent to Cavg-based titration (87%). Safety profiles were similar in both groups, but oral TU was associated with a mean increase in systolic BP of 3 to 5 mm Hg. Conclusion: A new oral TU formulation effectively restored T to mid-eugonadal levels in hypogonadal patients.
Testosterone undecanoate in the treatment of male hypogonadism
Expert Opin Pharmacother 2010 Aug;11(12):2095-106.PMID:20642374DOI:10.1517/14656566.2010.505920.
Importance of the field: Testosterone undecanoate (TU) represents an exciting new testosterone replacement therapy for hypogonadal men due to its convenient dosing schedule and favorable pharmacokinetic and safety profiles. Areas covered in this review: Clinical, pharmacokinetic and safety characteristics of TU will be reviewed. The characteristics of currently approved testosterone therapies will be reviewed and compared with those of TU in order to determine which therapy most appropriately meets the clinical objective of properly matching a patient with a therapy that is best able to deliver physiological levels of testosterone for prolonged periods of time, while at the same time being safe, effective, inexpensive, simple to use, and with few side effects. What the reader will gain: TU represents the first long-acting injectable with an excellent safety profile that can be administered only four times annually to produce stable levels of testosterone. Long-term studies have validated the clinical efficacy of TU in maintaining therapeutic levels of testosterone. Patient preference for the convenient dosing schedule might also lead to better compliance and therapeutic benefit. No serious side effects have been noted with the use of TU, including long-term data on patients treated with TU over 8 years. Take home message: TU is both a desirable and safe option for the treatment of hypogonadal men. Patients will benefit from the stable testosterone levels and fewer required injections, while achieving the desired benefits of androgen replacement.
Injectable Testosterone undecanoate for the treatment of hypogonadism
Expert Opin Pharmacother 2014 Sep;15(13):1903-26.PMID:25080279DOI:10.1517/14656566.2014.944896.
Introduction: Injectable Testosterone undecanoate (TU) is a long-acting testosterone (T) formulation available for the treatment of male hypogonadism (HG) since 2003. Areas covered: The efficacy and safety of injectable TU are assessed, as obtained by meta-analyzing available evidence. An extensive Medline, Embase and Cochrane search was performed. All uncontrolled and placebo-controlled randomized clinical trials (RCTs), evaluating the effect of injectable TU on different outcomes, were included. Of the 98 retrieved articles, 33 were included in the study. Among those, 11 were placebo-controlled RCTs. Injectable TU was significantly associated with a reduction of fat mass and HbA1c in both controlled and uncontrolled trials, in particular when hypogonadal subjects were enrolled. Similar results were observed for the improvement of erectile function. In addition, TU ameliorated several other outcomes, including blood pressure, lipid profile, waist circumference and body mass index in uncontrolled studies, but these data were not confirmed in placebo-controlled trials. The treatment was well tolerated and no risk of prostate cancer or cardiovascular disease was observed. Expert opinion: Injectable TU is a safe and effective treatment for male HG. The possibility of a therapeutic intervention just four to five times per year frees the patient, at least partially, from having a chronic condition, thus maintaining a positive, active role in self-caring.
Occurrence of pulmonary oil microembolism (POME) with intramuscular Testosterone undecanoate injection: literature review
Int J Impot Res 2022 May 24.PMID:35610506DOI:10.1038/s41443-022-00585-1.
Testosterone undecanoate injections (TU), an oil-based depot, is a universal hormonal-based treatment which has been associated with pulmonary oil microembolism (POME). However, the rate of POME during routine intramuscular (IM) TU injection is unknown. Here, we conduct a peer-reviewed literature review investigating POME incidents in the setting of TU injections. A total of 48 articles were selected in the literature review, which included 29 studies that used TU and reported its effects. Relatively few POME cases were reported across multiple published studies, including those that focused particularly on the occurrence rate of POME while administrating IM TU. Of the 29 individual studies, which included 7 978 patients, eight studies reported a total of 88 incidence of POME cases or cough. This included episodes of cough that were not originally declared as POME. One post market review reported 223 cases per 3,107,652 injections. When POME did occur, almost all cases resolved spontaneously within 60 min without intervention. Overall, POME was observed to be rare.