Deslorelin (acetate)
(Synonyms: D-Trp6-Pro9-des-Gly10-GnRH ethylamide, pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHEt) 目录号 : GC49143
A peptide agonist of GnRH
Cas No.:1642579-30-3
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
Deslorelin is a peptide agonist of gonadotropin-releasing hormone (GnRH).1 It binds to the GnRH receptor (GnRHR) with a Ki value of 0.1 nM. Deslorelin decreases testicular volume, semen volume, sperm motility, and total sperm count, as well as increases the percentage of abnormal sperm, in dogs when administered via a subcutaneous implant at doses of 3, 6, and 12 mg/kg.2 It decreases disease severity and plasma levels of estradiol, 17-hydroxyprogesterone, and androstenedione in ferrets with adrenocortical disease (ACD) when administered at doses ranging from 3 to 4.41 mg/kg per implant.3 Deslorelin (4.7 mg/implant per animal) suppresses ovulation and estrus in cats.4 Formulations containing deslorelin have been used in the management of ACD in ferrets and ovulation regulation and artificial insemination in horses.
1.Nederpelt, I., Georgi, V., Schiele, F., et al.Characterization of 12 GnRH peptide agonists - a kinetic perspectiveBr. J. Pharmacol.173(1)128-141(2016) 2.Junaidi, A., Williamson, P.E., Martin, G.B., et al.Dose-response studies for pituitary and testicular function in male dogs treated with the GnRH superagonist, deslorelinReprod. Domest. Anim.44(5)725-734(2009) 3.Wagner, R.A., PichÉ, C.A., JÖchle, W., et al.Clinical and endocrine responses to treatment with deslorelin acetate implants in ferrets with adrenocortical diseaseAm. J. Vet. Res.66(5)910-914(2005) 4.Ackermann, C.L., Volpato, R., Destro, F.C., et al.Ovarian activity reversibility after the use of deslorelin acetate as a short-term contraceptive in domestic queensTheriogenology78(4)817-822(2012)
| Cas No. | 1642579-30-3 | SDF | |
| 别名 | D-Trp6-Pro9-des-Gly10-GnRH ethylamide, pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHEt | ||
| Canonical SMILES | OC(C=C1)=CC=C1C[C@H](NC([C@H](CO)NC([C@@H](NC([C@@H](NC([C@H]2NC(CC2)=O)=O)CC3=CN=CN3)=O)CC4=CNC5=CC=CC=C45)=O)=O)C(N[C@@H](C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N6[C@@H](CCC6)C(NCC)=O)=O)=O)=O)CC7=CNC8=CC=CC=C78)=O.CC(O)=O | ||
| 分子式 | C64H83N17O12·XC2H4O2 | 分子量 | 1282.5 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 5 mg/ml,Ethanol: 10 mg/ml | 储存条件 | -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 | 0.7797 mL | 3.8986 mL | 7.7973 mL |
| 5 mM | 0.1559 mL | 0.7797 mL | 1.5595 mL |
| 10 mM | 0.078 mL | 0.3899 mL | 0.7797 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。
[The use of Deslorelin acetate (Suprelorin®) in companion animal medicine]
Schweiz Arch Tierheilkd 2012 Jan;154(1):7-12.PMID:22222897DOI:10.1024/0036-7281/a000286.
In 2009 Suprelorin® was released in Switzerland for the temporary suppression of fertility in male dogs. However, in practice it has also been used to treat other conditions in male dogs and in bitches. These include treatment of benign hyperplasia of the prostate, the induction or suppression of oestrus and treatment for the side effects of gonadectomy. Also in feline reproductive medicine GnRH-agonists gain increased importance. These areas of application are listed here in terms of treatment success and possible adverse effects after treatment of which owners have to be informed beforehand.
Sustained-release Deslorelin acetate implants disrupt oestrous cyclicity in the mare
Aust Vet J 2023 Apr 16.PMID:37062896DOI:10.1111/avj.13244.
There is a need for a safe, effective and practical method of oestrus suppression in the mare. The aim of this study was to monitor ovarian activity in mares exposed to either 9.4 or 28.2 mg Deslorelin acetate, a GnRH agonist, in the form of a sustained-release implant. Following oestrus synchronisation, mares were randomly assigned to one of three groups (n = 4 per group) and administered either one (Des1 group; 9.4 mg) or three (Des3 group; 28.2 mg) implants of Deslorelin acetate (Suprelorin-12, Virbac Australia) or one blank implant (Control group; Virbac Australia). Mares underwent weekly blood sampling for 12 weeks following implant placement (Day 0-Day 84), with transrectal palpation and ultrasonography of the reproductive tract at all sampling timepoints except Days 56, 70 and 77. All mares showed baseline serum progesterone concentrations (SPC; ≤1.3 nmol/L or 0.4 ng/ml) on Day 0. Cycling Control mares showed typical oestrous cyclicity characterised by peaks and troughs in SPC over time. Four of eight treated mares demonstrated a sustained elevation in SPC after the initial ovulation after implant placement; SPC declined to baseline levels (Des1 group; 2 mares) or remained elevated (Des3 group; 2 mares) at the final sampling timepoint on Day 84. Oestrous cyclicity was erratic in three of the remaining four treated mares. In total, 87.5% (7 of 8) of treated mares showed atypical oestrous cyclicity after implant placement. These results suggest that Deslorelin acetate disrupts oestrous cyclicity in the mare, which warrants further research.
A Comparative Study of the Effects of Osaterone acetate and Deslorelin acetate on Sperm Kinematics and Morpho-Functional Parameters in Dogs
Animals (Basel) 2022 Jun 15;12(12):1548.PMID:35739884DOI:10.3390/ani12121548.
Benign prostatic hyperplasia (BPH) is one of the most common problems in older male dogs that often has a huge impact on their health and welfare. This article presents a comparison between osaterone acetate (Ypozane®; Virbac®)(OA) and Deslorelin acetate (Suprelorin®; Virbac®)(DA), medications that are the main therapeutic alternative to castration in dogs with BPH. Forty dogs were divided into four groups: I-negative control (five dogs without BPH); II-positive control (10 individuals diagnosed with BPH); III-15 dogs treated with DA, and IV-10 individuals treated with OA. Semen fractions were collected on days 0 (day of treatment), 7, 14, and 21, and weeks 8, 12, 16, and 20. Macroscopic, microscopic and CASA analyses were performed. Both DA and OA significantly affected the properties of the canine ejaculate. The DA lead to the lack of libido and had lesser effects to the sperm function before it caused azoospermia, whereas OA had no effect on libido and only temporary reduction in seminal plasma volume was observed, which resulted in temporary deterioration in the percentage of motile and progressive spermatozoa.
Long-term effects of GnRH agonists on fertility and behaviour
Reprod Domest Anim 2017 Apr;52 Suppl 2:336-347.PMID:28025851DOI:10.1111/rda.12898.
This review aimed to summarize the present knowledge about the effects of GnRH agonist slow-release implants (GnRH A-SRI) on fertility and behaviour in male and female dogs and cats with special focus on Deslorelin. Following an initial stimulation of gonadotropin and testosterone secretion possibly associated with an improved semen quality, GnRH A-SRI induce long-term depression of fertility in male dogs and cats with, however, a large individual variation in onset and duration of efficacy especially in cats. The GnRH A-SRI furthermore interfere with testosterone-dependent/affected behaviour; a significant positive effect in reducing sexual behaviour and libido, hypersexuality, intermale dominance and excessive territorial urine marking has been described. Rates of improvement of the respective behaviour are comparable to those after surgical castration, making GnRH A-SRI a valuable option to predict castration-related effects on behaviour and to identify animals where surgical castration will not be beneficial. No effect has been seen in reducing aggression towards humans indicating the need for behavioural therapy to control this problem. Effects on spermatogenesis, steroidogenesis and behaviour have by now been shown to be fully reversible. Knowledge in females is more limited, and particularly, the initial induction of a possibly fertile oestrus and individual variation in duration of efficacy remain problems in bitches and queens treated for suppression of fertility. However, long-term suppression of oestrous cycle and fertility seems to be possible with induced effects shown to be reversible including restoration of normal fertility after the end of efficacy/GNRH A-SRI removal.
Long-term effect of repeated Deslorelin acetate treatment in bitches for reproduction control
Theriogenology 2021 Oct 1;173:73-82.PMID:34339906DOI:10.1016/j.theriogenology.2021.07.015.
Long-acting gonadotropin-releasing hormone (GnRH) analogs, which are approved for male dogs and ferrets, have been used off-label to suppress estrus in bitches predisposed to the side effects of spaying. Health data from the past 12 years were evaluated from bitches without progestogen pretreatment that received Deslorelin acetate (DA) to suppress estrus for the first time before the age of 4.5 years. The study population included 32 client-owned bitches repeatedly treated with either 4.7 mg or 9.4 mg DA implants for a period of 5.3 ± 3.4 years (range 0.5-11.3 years). Follow-up information concerning immediate side effects of DA occurring within five months after the first DA treatment (n = 23) as well as long-term side effects of sustained gonadal suppression occurring after five months up to three years (n = 2), three years up to five years (n = 2) or more than five years (n = 8) were assessed through a questionnaire. Treatment was considered successful if no major side effects requiring medical treatment occurred, which applied to 26 out of 32 (81 %) bitches. In the six remaining bitches, the following major side effects led to treatment discontinuation: persistent urinary incontinence (n = 1), reoccurring induced heat (n = 1), uterine disease (n = 3) and/or ovarian tumor (n = 3). The bitches recovered completely after surgical spaying and/or DA implant removal. Minor side effects that did not require therapy or affect animal welfare included body weight changes (n = 18), subtle behavioral changes (n = 13), induced heat (n = 12), coat changes (n = 11), pseudocyesis (n = 6), transient urinary incontinence (n = 4), and/or temporary thickening of the uterine wall with little anechogenic content (n = 2). To examine a possible causal relationship between adverse side effects and DA treatment, further studies should compare the frequency of pathologies between groups of GnRH-treated, intact and spayed bitches of similar breeds and ages. Nevertheless, DA application before the age of 4.5 years may be a means of postponing surgical spaying for several years in breeds at high risk for developing urinary incontinence. Before DA is used in bitches, owners should be fully informed regarding possible side effects.