Histrelin (acetate)
(Synonyms: 醋酸组氨瑞林) 目录号 : GC43866
A synthetic GNRH agonist
Cas No.:220810-26-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor). It stimulates release of oxytocin and vasopressin ex vivo from the isolated rat hypothalamo-neurohypophysial system at a concentration of 100 nM. In vivo, the initial dose of histrelin (100 μg) stimulates acute increases in luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone serum levels (50-, 2.5-, and 15-fold, respectively), while chronic treatment leads to 95% decreases in LH and FSH responses in rhesus monkeys. Formulations containing histrelin have been used in the treatment of advanced prostate cancer and central precocious puberty.
| Cas No. | 220810-26-4 | SDF | |
| 别名 | 醋酸组氨瑞林 | ||
| Canonical SMILES | O=C([C@@H]1CCC(N1)=O)N[C@@H](CC2=CNC=N2)C(N[C@@H](CC3=CNC4=C3C=CC=C4)C(N[C@@H](CO)C(N[C@@H](CC5=CC=C(O)C=C5)C(N[C@H](CC6=CN(CC7=CC=CC=C7)C=N6)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N8CCC[C@H]8C(NCC)=O)=O)=O)=O)=O)=O)=O)=O.OC(C)=O | ||
| 分子式 | C66H86N18O12•XC2H4O2 | 分子量 | 1323.5 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 0.25 mg/ml,PBS (pH 7.2): 10 mg/ml | 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 | 0.7556 mL | 3.7779 mL | 7.5557 mL |
| 5 mM | 0.1511 mL | 0.7556 mL | 1.5111 mL |
| 10 mM | 0.0756 mL | 0.3778 mL | 0.7556 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。
Histrelin acetate-induced ovulation in Brazilian Northeastern jennies (Equus asinus) with different follicle diameters
Theriogenology 2019 Sep 15;136:95-100.PMID:31254727DOI:10.1016/j.theriogenology.2019.06.037.
The aim of the present study was to evaluate the efficacy of a GnRH analog for induction of ovulation in Brazilian Northeastern jennies (Equus asinus) with different follicle diameters. Four consecutive estrus of 10 jennies were used in a crossover study; C (Control, n = 10) jennies were evaluated by transrectal palpation and ultrasonography until a spontaneous ovulation and the intervals between the predetermined follicular size (25-28 mm [C1], 29-32 mm [C2] and 33-36 mm [C3] follicle) and ovulation were registered. In treated cycle, jennies had the ovulation induced by 250 μg of Histrelin acetate (Strelin®, Botupharma, Botucatu, Brazil) when respective follicle diameters 25-28 mm (T1), 29-32 mm (T2) and 33-36 mm (T3) were diagnosed. Ovulation was monitored by transrectal palpation and ultrasonography. Different follicle diameters significantly affected (P < 0.05) the interval until ovulation between control and matched treated cycles. Interval between prostaglandin administration and ovulation diagnosis was lower in jennies from T2 group (145.2 ± 34.6 h) compared with the control cycle (220.0 ± 41.8 h) and also with other treated cycles (T1 - 209.8 ± 48.0 h; T3 - 183.3 ± 33.9 h). Histrelin acetate treatment also reduces the interval between detection of predetermined follicular size and ovulation (P < 0.05) in all treated cycles groups compared with matched control group. Higher percentage (P < 0.05) of jennies had success of ovulation induction (36-48 h after Histrelin acetate injection) in all treated cycles in contrast with the matched control group. In addition, in comparison among treated cycle groups, more (P < 0.05) jennies (100%) in T2 ovulated between 36 and 48 h after ovulation induction, compared with T1 and T3, which did not differ (P > 0.05) from each other. Edema scoring and ovulation were not associated events (r = 0.0219). In conclusion, jennies with 29-32 mm follicles satisfactory responded to ovulation induction with Histrelin acetate, which allowed the shortening of interovulatory interval in all groups evaluated.
Histrelin: in advanced prostate cancer
Drugs 2010 Mar 26;70(5):623-30.PMID:20329807DOI:10.2165/11204800-000000000-00000.
Histrelin is a gonadotropin-releasing hormone agonist available in a diffusion-controlled reservoir drug delivery system for subcutaneous implantation. The subcutaneous Histrelin implant provided sustained suppression of serum testosterone, luteinizing hormone (LH) and prostate-specific antigen levels for up to 1 year in patients with advanced prostate cancer in two phase II or III trials. In the noncomparative, multicentre, phase III study, serum testosterone was suppressed to castrate levels (i.e. < or =50 ng/dL) within 4 weeks in all patients who received a Histrelin acetate 50 mg implant, with 99-100% of Histrelin implant recipients maintaining castrate levels for the remainder of the 1-year treatment period. Such efficacy was provided irrespective of patient age or stage of disease. Although a transient surge in serum testosterone levels occurred after placement of the initial Histrelin implant, no acute elevations in testosterone or LH levels were observed in patients whose implant was replaced after 1 year of therapy and suppression of these hormones continued to be maintained. The Histrelin implant was generally well tolerated in patients with advanced prostate cancer in the phase III trial and in a pooled analysis. No patients prematurely discontinued treatment because of adverse events, most of which were the consequence of hormone suppression.
Clinical characteristics and treatment patterns with Histrelin acetate subcutaneous implants vs. leuprolide injections in children with precocious puberty: a real-world study using a US claims database
J Pediatr Endocrinol Metab 2021 Jun 21;34(8):961-969.PMID:34147047DOI:10.1515/jpem-2020-0721.
Objectives: Gonadotropin-releasing hormone analogs are the treatment of choice for central precocious puberty (CPP). This study characterizes patients treated with Histrelin implant or leuprolide injection. Methods: A US claims database was used to identify patients aged ≤20 years with ≥1 Histrelin or leuprolide claim (index treatment) between April 2010 and November 2017 and continuous enrollment ≥3 months before and ≥12 months after the index treatment date. Results: Overall, 4,217 patients (Histrelin, n=1,001; leuprolide, n=3,216) were identified. The percentage of patients with CPP diagnosis was greater in the Histrelin (96.5%) vs. leuprolide (68.8%; p<0.0001) cohort. In patients with CPP (Histrelin, n=966; leuprolide, n=2,214), mean age at treatment initiation was similar for Histrelin (9.0 ± 2.0 years) and leuprolide (9.1 ± 2.3 years), with >50% of patients aged 6-9 years. Mean treatment duration was significantly longer for Histrelin (26.7 ± 14.8 months) vs. leuprolide (14.1 ± 12.1 months; p<0.0001), and was longer in younger patient groups. More patients switched from leuprolide to Histrelin (12.3%) than vice versa (3.6%; p<0.0001). Median annual total treatment costs were slightly lower for the Histrelin cohort ($23,071 [interquartile range, $16,833-$31,050]) than the leuprolide cohort ($27,021 [interquartile range, $18,314-$34,995]; p<0.0001). Conclusions: Patients with CPP treated with Histrelin had a longer duration of treatment, lower rates of index treatment discontinuation, and lower annual treatment costs vs. those treated with leuprolide.
Comparative Efficacy of Histrelin acetate and hCG for Inducing Ovulation in Brazilian Northeastern Jennies (Equus africanus asinus)
J Equine Vet Sci 2020 Sep;92:103146.PMID:32797776DOI:10.1016/j.jevs.2020.103146.
The goal of this study was to compare the efficiency of Histrelin acetate (GnRH analog) and human chorionic gonadotropin (hCG) to hasten ovulation in Brazilian Northeastern jennies (Equus africanus asinus). Thirty cycles of ten jennies were randomly assigned in one of the three groups: G0 (control group), saline; G1, 250 μg of Histrelin acetate; G2, 2500 IU of hCG. Jennies were evaluated by transrectal palpation and ultrasonography, and had the administration of an ovulation-inducing agent when a follicle measuring between 29 and 32 mm of diameter was diagnosed. Jennies were monitored every 6 hours by transrectal ultrasonography until ovulation. The interval between prostaglandin administration and ovulation was lower (P < .05) in jennies from the G1 (145.2 ± 34.6 hours) and G2 (147.4 ± 27.3 hours) groups compared with the control cycle (220.0 ± 41.8 hours). Both treatments (G1, 41.15 ± 3.5 hours; G2, 37.8 ± 2.5 hours) also reduced (P < .05) the interval that jennies took to ovulate after the administration of the ovulation-inducing agent compared with the control (81.8 ± 28.8 hours). All jennies from G1 and G2 ovulated up to 48 hours after ovulation induction, whereas 100% of jennies in the control cycle ovulated later (>48 hours from the administration of saline). In conclusion, both Histrelin acetate and hCG at the used dose are efficient ovulation-inducing agents in jennies promoting ovulation up to 48 hours after administration.
[Histrelin acetate--the first once yearly LHRH agonist]
Lijec Vjesn 2011 Sep-Oct;133(9-10):320-2.PMID:22165080doi
Long-acting synthetic luteinising hormone-releasing hormone agonists have become the mainstay for androgen-deprivation therapy, because they avoid the physical and psychological discomfort associated with orchidectomy and lack the potential cardiotoxicity associated with estrogens such as diethylstilbestrol. Currently available luteinising hormone-releasing hormone agonist analogues include leuprolide, goserelin, triptorelin, degarelix and buserelin were administered as either intramuscular or subcutaneous depot injections on a 1, 2, 3 or 6 months basis. Histrelin acetate is the first long-acting luteinising hormone-releasing hormone agonist available as a once-yearly subcutaneous implant.