Fertirelin Acetate is a synthetic peptide that promotes ovulation and fertility. Purchase Fertirelin research peptide for breeding and hormonal studies.
CAT No: 10-101-17
CAS No:38234-21-8 (net)
Synonyms/Alias:(Des-Gly10,Pro-NHEt9)-LHRH; Fertirelin; Fertirelina; Fertireline; Fertirelinum
Chemical Name:acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Fertirelin Acetate is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), designed to mimic the activity of endogenous GnRH in stimulating the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary. As a member of the peptide hormone family, Fertirelin Acetate features a modified amino acid sequence that enhances its resistance to enzymatic degradation and prolongs its biological activity compared to natural GnRH. Its high receptor affinity and well-characterized mechanism of action make it a valuable tool in neuroendocrine research, reproductive biology, and studies focusing on the hypothalamic-pituitary-gonadal (HPG) axis. The synthetic nature and stability of this decapeptide render it particularly useful for controlled laboratory applications requiring precise modulation of gonadotropin release.
Reproductive Endocrinology Research: Fertirelin Acetate is widely utilized as a research tool for investigating the regulatory mechanisms governing the HPG axis. By acting as a potent agonist at GnRH receptors, it enables researchers to induce and study the downstream secretion of LH and FSH in vitro and in vivo. This facilitates the elucidation of feedback mechanisms, signal transduction pathways, and receptor desensitization processes integral to reproductive endocrinology. Its application is instrumental in dissecting the molecular dynamics of gonadotropin release and the physiological responses of pituitary gonadotrophs to GnRH stimulation.
Peptide Structure-Function Studies: The unique sequence and enhanced stability of Fertirelin Acetate make it an important model in peptide structure-function analysis. Researchers employ this analog to compare the biological activity and receptor interaction profile of native GnRH versus synthetic derivatives. Such studies provide insights into the influence of specific amino acid substitutions on receptor binding affinity, agonist potency, and metabolic stability, thereby advancing the rational design of novel GnRH analogs with tailored pharmacological properties.
Signal Transduction Analysis: Fertirelin Acetate serves as a reliable probe for dissecting GnRH receptor-mediated signaling pathways in pituitary and extrapituitary tissues. Its ability to reproducibly activate GnRH receptors allows for detailed examination of downstream effectors such as phospholipase C, protein kinase C, and intracellular calcium mobilization. This application is critical for mapping the cascade of molecular events triggered by GnRH receptor engagement and for identifying modulators or inhibitors of these pathways in various cellular contexts.
Endocrine Disruption Assessment: The compound is also employed in studies evaluating the impact of endocrine-disrupting chemicals (EDCs) on the HPG axis. By providing a standardized stimulus for gonadotropin release, Fertirelin Acetate enables researchers to assess how environmental contaminants or test compounds alter GnRH receptor responsiveness and pituitary function. This approach is essential for toxicological screening and for understanding the mechanisms by which EDCs interfere with reproductive hormone regulation.
Peptide Receptor Pharmacology: In pharmacological research, Fertirelin Acetate is used to characterize the binding kinetics, specificity, and functional responses of GnRH receptor subtypes across different species or tissue types. Its high potency and stability make it ideal for dose-response studies, receptor desensitization assays, and competitive binding experiments. These investigations contribute to the broader understanding of peptide hormone receptor pharmacology and support the development of new peptide-based modulators for experimental use in neuroendocrine systems.
The effect of using a dose of 50 micro g rather than 100 micro g fertirelin in an ovulation/fixed-time insemination protocol for Holstein-Friesian dairy cows was investigated in three experiments. In each experiment, fertirelin was administered at the beginning of the protocol followed 7 days later by 500 micro g cloprosterol. Two days later, a second dose of fertirelin was given and AI performed 16-19 h later regardless of the incidence of behavioral oestrus. The effect on conception rate was studied in experiment 1 using 114 postpartum anoestrus cows. There was no significant difference in the age, parity or number of days after parturition in each treatment groups. The conception rate did not differ between the 50 micro g fertirelin group (61.1%; n=72) and the 100 micro g group (59.5%; n=42; NS). In experiment 2, a further 12 cows at 40-60 days postpartum were treated with 100 or 50 micro g fertirelin (n=6 per dose) with treatment commencing in the follicular or luteal phase of the oestrous cycle. The plasma concentration of luteinizing hormone (LH) reached similar peaks of over 5 ng/ml 120 min after the intramuscular administration of fertirelin in both groups. There were no significant differences in LH levels between treatments or phase of the oestrous cycle when treatment commenced. Doses of 50 and 100 micro g fertirelin were compared in experiment 3 using 17 cows to study follicular wave development and synchronization by transrectal ultrasonography, conception rate and corpus luteum function. There were no significant differences between treatments for these factors. It was concluded that using a dose of 50 micro g fertirelin enabled the drug costs to be reduced without affecting the efficiency of a synchronization of ovulation/fixed-time AI protocol for dairy cows.
Yamada, K., Nakao, T., Nakada, K., & Matsuda, G. (2002). Influence of GnRH analogue (fertirelin acetate) doses on synchronization of ovulation and fixed-time artificial insemination in lactating dairy cows. Animal reproduction science, 74(1), 27-34.
The optimum dose for establishing superovulation in mice of Fertirelin Acetate (FA), an LH-RH analogue, was examined. Mice were subcutaneously injected with 5 IU of hCG at 17:00 (Day 0), and with various doses of FA (0.001 to 1.0 microg) five times at 4 h intervals on and after 22:00 on Day 0. To induce ovulation, 5 IU of hCG was again injected subcutaneously at 17:00 on Day 2. In the groups administered with doses ranging from 0.01 to 0.5 microg of FA, the number of ovulated eggs was significantly (p<0.05) larger than in the control group (12.9 +/- 5.9). The greatest number of ovulated eggs (22.6 +/- 7.3) was obtained in the group administered with 0.025 microg of FA. The results indicate that the effective dose of LH-RH analogue, FA, is between 0.1 and 0.5 microg for superovulation induction in mice.
Nariai, K., Ishinazaka, T., Suzuki, K., UCHIYAMA, H., SATO, K., ASANO, R., ... & KANAYAMA, K. (2005). Optimum dose of LH-RH analogue Fertirelin Acetate for the induction of superovulation in mice. Experimental animals, 54(1), 97-99.
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