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Deslorelin Acetate

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CAT#
10-101-10
Synonyms/Alias
(Des-Gly10,D-Trp6,Pro-NHEt9)-LHRH; Ovuplant; Somagard
CAS No.
57773-65-6 (net)
Sequence
Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHEt acetate salt
M.W/Mr.
1281.64
Molecular Formula
C64H83N17O12
Source
Synthetic
Long-term Storage Conditions
−20°C
Application
Deslorelin Acetate (brand name Ovuplant) is currently approved for use in veterinary medicine and is used to induce ovulation in mares as part of the artificial insemination process. It is also used to stabilize high-risk pregnancies, mainly of livestock.
Description
Deslorelin acetate is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist) also known as an LHRH agonist. It stops the production of sex hormones (testosterone and oestrogen).
Areas of Interest
Hormonal therapy
  • Background
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Deslorelin Acetate is a synthetic nonapeptide analogue of the natural gonadotrophin releasing hormone (GnRH) with potential antineoplastic activity. Deslorelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Continuous, prolonged administration of goserelin in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.

CAS: 16679-58-6
Sequence: 3-Mercaptopropionyl-Tyr-Phe-Gln-Asn-Cys-Pro-D-Arg-Gly-NH2 acetate salt (Disulfide bond)
M.W: 1069.2
Molecular Formula: C46H64N14O12S2
CAS: 38234-21-8 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-NHEt acetate salt
M.W: 1153.31
Molecular Formula: C55H76N16O12
CAS: 123246-29-7
Sequence: Ac-DNal-DCpa-DPal-Ser-Tyr-DHar(Et2)-Leu-Har(Et2)-Pro-DAla -NH2
M.W: 1570.4
Molecular Formula: C80H113ClN18O13
CAS: 34973-08-5
Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 acetate salt
M.W: 1242.36
Molecular Formula: C55H75N17O13.C2H4O2
CAS: 33515-09-2 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 hydrochloride salt
M.W: 1182.31
Molecular Formula: C55H75N17O13

A 2-year-old female ovariectomised Norwegian Forest cat with a history of post-spaying urinary incontinence was diagnosed with acquired urinary sphincter mechanism incompetence (USMI) after complete clinical and laboratory examination. Although there is no literature regarding the treatment of post-spaying USMI in cats, deslorelin acetate is successful in the treatment of post-spaying USMI in dogs. Deslorelin acetate implants have been shown previously to be effective for contraception and oestrus suppression in queens, and suppression of reproductive function in tomcats. Therefore, deslorelin acetate implant treatment was chosen for treatment of post-spaying USMI in this queen. Follow-up examinations were performed on days 8, 15 and 30 after deslorelin implant insertion. Urinary continence was restored about 25 days after implantation and maintained for at least 15 months, without treatment-related negative effects. In the present case report, the post-spaying urinary incontinence related to the acquired USMI was successfully treated with a deslorelin acetate implant. In addition, safe implantation was easy in cats and the single injection resulted in long-lasting efficacy. Further studies are needed to confirm the usefulness of deslorelin acetate treatment for post-spaying USMI in queens and to better delineate the duration of efficacy.

Pisu, M. C., & Veronesi, M. C. (2014). Effectiveness of deslorelin acetate subcutaneous implantation in a domestic queen with after-spaying urinary incontinence. Journal of feline medicine and surgery, 16(4), 366-368.

Compared with findings before deslorelin treatment, vulvar swelling, pruritus, sexual behaviors, and aggression were significantly decreased or eliminated within 14 days of implantation; hair regrowth was evident 4 to 6 weeks after treatment. Within 1 month of treatment, plasma hormone concentrations significantly decreased and remained decreased until clinical relapse. Mean time to recurrence of clinical signs was 13.7 +/- 3.5 months (range, 8.5 to 20.5 months). In 5 ferrets, large palpable tumors developed within 2 months of clinical relapse; 3 of these ferrets were euthanatized because of adrenal gland tumor metastasis to the liver or tumor necrosis.

Wagner, R. A., Piché, C. A., Jöchle, W., & Oliver, J. W. (2005). Clinical and endocrine responses to treatment with deslorelin acetate implants in ferrets with adrenocortical disease. American journal of veterinary research, 66(5), 910-914.

Two adult, male domestic turkeys were treated with implants of deslorelin acetate, a gonadotropin-releasing hormone agonist, to reduce intermale aggression and aggression directed toward the animal care team at a zoologic institution. The turkeys were manually restrained and either two 4.7-mg or two 9.4-mg implants were placed within the pectoral musculature on 3 occasions over the course of approximately 1.5 years. Plasma testosterone concentrations were measured by radioimmunoassay every 2 weeks for the first month after a new implant placement and then monthly thereafter. Testosterone concentrations remained low and aggressive behavior was decreased for a period of several months after implant placement. At necropsy of both birds, no adverse gross or histologic lesions were noted at the implantation sites in the pectoral musculature or within the gonadal tissue. Deslorelin acetate implants are a treatment modality to consider for mitigation of aggression in male domestic turkeys.

Molter, C. M., Fontenot, D. K., & Terrell, S. P. (2015). Use of deslorelin acetate implants to mitigate aggression in two adult male domestic turkeys (Meleagris gallopavo) and correlating plasma testosterone concentrations. Journal of avian medicine and surgery, 29(3), 224-230.

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