Triptorelin acetate
(Synonyms: 醋酸曲普瑞林) 目录号 : GC34012
Triptorelinacetate是促性腺激素释放激素受体(GnRH)激动剂。
Cas No.:140194-24-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Triptorelin acetate is a Gonadotropin-releasing hormone receptor (GnRH) agonist.
[1]. Jiang J, et al. Efficacy and Safety of gonadotropin-releasing hormone (GnRH) Agonists Triptorelin Acetate and Cetrorelix Acetate in Assisted Reproduction. Med Sci Monit. 2018 Nov 8;24:7996-8000.
| Cas No. | 140194-24-7 | SDF | |
| 别名 | 醋酸曲普瑞林 | ||
| Canonical SMILES | O=C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N(CCC1)[C@@H]1C(NCC(N)=O)=O)=O)=O)[C@H](NC([C@@H](NC([C@H](CO)NC([C@@H](NC([C@@H](NC([C@H](CC2)NC2=O)=O)CC3=CNC=N3)=O)CC4=CNC5=C4C=CC=C5)=O)=O)CC6=CC=C(O)C=C6)=O)CC7=CNC8=C7C=CC=C8.CC(O)=O | ||
| 分子式 | C66H86N18O15 | 分子量 | 1371.5 |
| 溶解度 | Soluble in DMSO | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.7291 mL | 3.6456 mL | 7.2913 mL |
| 5 mM | 0.1458 mL | 0.7291 mL | 1.4583 mL |
| 10 mM | 0.0729 mL | 0.3646 mL | 0.7291 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。
Triptorelin acetate (Veterinary Medicinal Products)
Food Saf (Tokyo) 2016 Dec 22;4(4):173-174.PMID:32231921DOI:10.14252/foodsafetyfscj.2016026s.
The Food Safety Commission of Japan (FSCJ) conducted a risk assessment of Triptorelin acetate (CAS No. 140194-24-7), which is intended for use in a single fixed-time insemination by synchronizing estrus cycles of weaned sows, based on the documents for the import tolerance application. FSCJ recognize none of adverse effects of Triptorelin acetate on human health through dietary exposure, because of the lack of genotoxicity relevant to human health and negligible oral bioavailability due to the degradation in the digestive tract. FSCJ thus judged it unnecessary to establish an acceptable daily intake (ADI) for Triptorelin acetate.
Comparison of Triptorelin acetate vs triptorelin pamoate in the treatment of Central precocious puberty (CPP): a retrospective study
Gynecol Endocrinol 2020 Apr;36(4):338-340.PMID:31441342DOI:10.1080/09513590.2019.1655726.
The aim of this study is to compare the clinical and biochemical outcomes of Triptorelin acetate (TPA) versus triptorelin pamoate (TPP) treatment in girls with central precocious puberty. A total of 60 patients with idiopathic CPP were retrospectively recruited. Thirty girls were treated with Triptorelin acetate 3.75 mg/month (TPA group) and thirty girls in a second group received triptorelin pamoate 3.75 mg/4 weeks (TPP group). Patient follow-up at 12 and 24 months included GnRH Test at 12 months and baseline LH at 24 months. Patients were monitored with pelvic ultrasound, X-Ray of the hand and wrist and anthropometric evaluations. A total of 60/60 girls showed a good response to both formulations. Significant reductions in basal and LH peaks, estradiol values, breast pubertal stage, progression of bone age and growth velocity rate after 12 months treatment were obtained in both groups, demonstrating the equivalence of the two formulations in regulating the hypothalamic-pituitary-gonadal (HPG) axis. Triptorelin pamoate provided a more effective and significant reduction in LH peak after 12 months in comparison with Triptorelin acetate more effective in reducing ovarian volume and endometrial thickness. Both formulations were equivalent, even though the LH peak was significantly lower in girls treated with triptorelin pamoate.
Triptorelin acetate administration in early pregnancy: case reports and review of the literature
Eur J Obstet Gynecol Reprod Biol 1998 Oct;80(2):143-9.PMID:9846657DOI:10.1016/s0301-2115(98)00109-2.
When using a long protocol with cycle day 23 gonadotrophin-releasing hormone agonists (GnRH-a) administration, an elevated estradiol level or a missed period 10-14 days after initiating pituitary downregulation should alert the physician to the possibility of a pregnancy. We report 4 pregnancies occurring during pituitary downregulation with Triptorelin acetate in 366 in-vitro fertilization (IVF) cycles resulting in 3 deliveries of 4 normal neonates at term and 1 first trimester abortion. This supports published data reporting a 1% spontaneous pregnancy incidence in women undergoing pituitary desensitization GnRH-a during the luteal phase prior to planned IVF treatment, a 15.9% abortion rate and a 1.7% malformation rate. Our cases together with other published data suggest that pregnancy outcome is not adversely affected by GnRH-a administration during the luteal phase of the conception cycle. However, long term follow-up of these babies is still lacking and the number of reported cases is too small adequately to rule out the possibility of any detrimental effect related GnRH-a administration in pregnancy.
Sustained In-Vivo Release of Triptorelin acetate from a Biodegradable Silica Depot: Comparison to Pamorelin® LA
Nanomaterials (Basel) 2021 Jun 16;11(6):1578.PMID:34208450DOI:10.3390/nano11061578.
Triptorelin acetate was encapsulated into silica microparticles by spray-drying a mixture of colloidal silica sol and Triptorelin acetate solution. The resulting microparticles were then combined with another silica sol containing silica nanoparticles, which together formed an injectable silica-triptorelin acetate depot. The particle size and surface morphology of the silica-triptorelin acetate microparticles were characterized together with the in vitro release of triptorelin, injectability and rheology of the final injectable silica-triptorelin acetate depot. In vivo pharmacokinetics and pharmacodynamics of the silica-triptorelin acetate depot and Pamorelin® were evaluated and compared in Sprague-Dawley male rats after subcutaneous administration. Serum samples up to 91 days were collected and the plasma concentrations of triptorelin and testosterone were analyzed with ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). In vivo pharmacokinetics showed that injections of the silica-triptorelin acetate depot gave 5-fold lower Cmax values than the corresponding Pamorelin® injections. The depot also showed a comparable sustained triptorelin release and equivalent pharmacodynamic effect as the Pamorelin® injections. Detectable triptorelin plasma concentrations were seen with the depot after the 91-day study period and testosterone plasma concentrations remained below the human castration limit for the same period.
Single injection of triptorelin or buserelin acetate in saline solution induces ovulation in mares the same as a single injection of hCG
Reprod Domest Anim 2020 Mar;55(3):374-383.PMID:31930759DOI:10.1111/rda.13632.
The aim of this study was to assess the efficacy of different doses of buserelin acetate and another GnRH agonist, Triptorelin acetate, in saline solution in a single subcutaneous injection, to induce ovulation of growing pre-ovulatory follicle in mare and compare it with the classical treatment of a single injection of hCG. The study is split into 3 experiments over different breeding seasons in the same stud with a random distribution of treatment. The first one was to compare the injection of 6 mg of buserelin with 1,500 IU of hCG; the second one consisted of comparing different doses of buserelin (6 mg and 3 mg); and the third one compared three different doses of buserelin (3, 2 and 1 mg), 0.1 mg of triptorelin with 1,500 IU of hCG as a control group. The results of all experiments showed the same efficacy between all treatments with mares ovulating between 24 and 48 hr after injection: experiment 1: hCG (78% n = 41) and buserelin 6 mg (90% n = 50); experiment 2: buserelin 6 mg (78,1% n = 192) and buserelin 3 mg (78% n = 341); and experiment 3: hCG (87% n = 106), buserelin 3 mg (84,7% n = 137), buserelin 2 mg (82,7% n = 104), buserelin 1 mg (87% n = 54) and triptorelin 0.1 mg (84,7% n = 72). In conclusion, this study contributes to erasing the dogma that has been established since 1975 that a single injection in solution without any long-acting excipient of a GnRH agonist cannot induce ovulation in the mare. This study also shows that a injection of 0.1 mg of triptorelin in solution is a good alternative for ovulation induction and is comparable to small doses of buserelin acetate in solution (1 mg) and 1,500 IU of the gold standard trigger hCG, mainly in countries where human formulation of buserelin is not available.