Testosterone cypionate一种油溶性的、具有较长消除半衰期的睾酮前体药物,是雄激素受体(AR)的激动剂。
Cas No.:58-20-8
Sample solution is provided at 25 µL, 10mM.
Testosterone cypionate is an oil-soluble testosterone prodrug with a long elimination half-life, acting as an androgen receptor (AR) agonist. Testosterone cypionate promotes protein anabolism, reduces protein catabolism, and increases erythropoiesis by activating the androgen receptor. Testosterone cypionate is primarily used to treat male low testosterone levels, hypogonadism, and cryptorchidism[1-4].
In vivo, Testosterone cypionate (0.3mg/ml, 1.5mg/ml, 3.0mg/ml; 0.1ml/10g) was administered as a single intramuscular injection to 6-8 week old male Swiss mice. Testosterone cypionate (3.0mg/ml) induced micronucleus formation and reduced the PCE/NCE ratio, resulting in genotoxicity and cytotoxicity[5]. Testosterone cypionate (15mg/kg) was administered subcutaneously once daily for 10 days to C57BL/6J male mice with severe controlled cortical impact traumatic brain injury. Testosterone cypionate improved mitochondrial calcium ion efflux and ATP synthesis efficiency, and downregulated molecular drivers of neurodegeneration[6].
References:
[1] Rivero MJ, Ory J, Diaz P, et al. Comparison of Hematocrit Change in Testosterone-deficient Men Treated With Intranasal Testosterone Gel vs Intramuscular Testosterone Cypionate: A Randomized Clinical Trial. J Urol. 2023 Jul;210(1):162-170.
[2] Ponce MB, Schauberger E, Connor E, et al. Delayed hypersensitivity reaction to testosterone cypionate injections. Contact Dermatitis. 2024 Oct;91(4):364-365.
[3] Pan MM, Kovac JR. Beyond testosterone cypionate: evidence behind the use of nandrolone in male health and wellness. Transl Androl Urol. 2016 Apr;5(2):213-9.
[4] Damião B, Rossi-Junior WC, Guerra FDR, et al. Anabolic steroids and their effects of on neuronal density in cortical areas and hippocampus of mice. Braz J Biol. 2021 Jul-Sep;81(3):537-543.
[5] Meireles JR, Oliveira SV, Costa-Neto AO, et al. Genotoxic and cytotoxic effects of testosterone cypionate (deposteron(®)). Mutat Res. 2013 May 15;753(2):72-5.
[6] Carteri RB, Kopczynski A, Rodolphi MS, et al. Testosterone Administration after Traumatic Brain Injury Reduces Mitochondrial Dysfunction and Neurodegeneration. J Neurotrauma. 2019 Jul 15;36(14):2246-2259.
Testosterone cypionate一种油溶性的、具有较长消除半衰期的睾酮前体药物,是雄激素受体(AR)的激动剂。Testosterone cypionate通过激活雄激素受体来促进蛋白质合成代谢、减少蛋白质分解代谢,并增加红细胞生成。Testosterone cypionate主要用于治疗男性低睾酮水平、性腺功能减退症和隐睾症的相关治疗[1-4]。
在体内,Testosterone cypionate(0.3mg/ml、1.5mg/ml、3.0mg/ml;0.1ml/10g)单次肌肉注射,用于处理6-8周龄雄性瑞士小鼠。Testosterone cypionate(3.0mg/ml)诱导了微核形成并降低了PCE/NCE比值,产生基因毒性和细胞毒性[5]。Testosterone cypionate(15mg/kg)每天一次皮下注射,持续10天,用于处理严重控制性皮质撞击创伤性脑损伤模型C57BL/6J雄性小鼠。Testosterone cypionate改善了小鼠的线粒体钙离子外排和ATP合成效率,下调了神经退行性变的分子驱动因子[6]。
| Animal experiment [1]: | |
Animal models | C57BL/6J mice |
Preparation Method | Mice were submitted to severe controlled cortical impact (CCI) traumatic brain injury. Testosterone cypionate (15mg/kg) or vehicle was administered subcutaneously daily starting 24 hours after injury for 10 days. Mice were sacrificed 10 days after CCI for neurochemical analysis of ipsilateral cortex. |
Dosage form | 15mg/kg; subcutaneous injection; daily for 10 days |
Applications | Testosterone cypionate administration improved mitochondrial Ca2+ extrusion through NCLX exchanger, enhanced ATP synthesis efficiency, reduced H2O2 production, and downregulated molecular drivers of neurodegeneration (including pTauSer396, alpha-Spectrin fragmentation, caspase-3 activation, and Bax/BCL-2 ratio) after traumatic brain injury. |
References: | |
| Cas No. | 58-20-8 | SDF | |
| 别名 | 环戊丙酸睾酮;1-睾酮环戊丙酸酯 | ||
| 分子式 | C₂₇H₄₀O₃ | 分子量 | 412.61 |
| 溶解度 | 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 | 2.4236 mL | 12.118 mL | 24.236 mL |
| 5 mM | 484.7 μL | 2.4236 mL | 4.8472 mL |
| 10 mM | 242.4 μL | 1.2118 mL | 2.4236 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。
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