Fertirelin acetate, It exists in the form of acetate, with a chemical formula of C57H80N16O14 and a molecular weight of 1213.34-1213.37. Its chemical structure has a specific amino acid sequence, such as {Glp}-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro- {ethylamide} , This unique structure endows it with biological activity similar to natural GnRH, but with some differences, making it have specific application value in the fields of medicine and veterinary medicine. It was first introduced to the market in Japan in 1981 for the treatment of various ovarian failure problems in cattle, and has since been applied in multiple countries and regions, although it may no longer be available in some areas. It has been sold in the market under brand names such as Ovalyse.
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Fertirelin Acetate COA
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| Certificate of Analysis | ||
| Compound name | Fertirelin acetate | |
| Grade | Pharmaceutical grade | |
| CAS No. | 66002-66-2 | |
| Quantity | 50g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202512090051 | |
| MFG | Dec 9th 2025 | |
| EXP | Dec 8th 2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.52% |
| Loss on drying | ≤1.0% | 0.41% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.80% |
| Single impurity | <0.8% | 0.37% |
| Total microbial count | ≤750cfu/g | 85 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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Fertirelin Acetate Information
| Chemical Formula: | C57H80N16O14 |
| Exact Mass: | 1213 |
| Molecular Weight: | 1213 |
| m/z: | 1213 (100.0%), 1214(61.6%), 1215 (18.7%), 1154 (5.9%), 1155 (3.5%), 1156 (2.5%), 1155 (2.5%), 1156 (1.5%), 1156 (1.0%) |
| Elemental Analysis: | C, 56.42; H, 6.65; N, 18.473; O, 18.46 |
In addition to clinical applications, fertirelin acetate also has important value in scientific research and industrial fields, mainly used as a tool drug or intermediate.
1. Research on the hypothalamic pituitary gonadal axis
Application scenario: It is an ideal tool drug for studying the function and signaling pathway of GnRH receptors. It can specifically activate pituitary GnRH receptors for exploring receptor structure, ligand binding properties, and downstream signaling mechanisms.
Research value: In cell experiments, it can induce a 10-20 fold increase in LH and FSH secretion, providing a reliable model for studying hormone secretion regulation. In animal experiments, it can be used to construct reproductive dysfunction models and evaluate the efficacy of new drugs.
2. Intermediate for peptide drug development
Industrial application: It is an important intermediate in the synthesis of peptide drugs, and specific amino acid sequences in its structure (such as carboxyl groups blocked by ethylamine) provide active sites for subsequent modifications. For example, longer acting GnRH analogs (such as goserelin) can be developed by replacing specific amino acids.
Market value: The global peptide drug market has exceeded 50 billion US dollars, and as a key intermediate, the annual demand reaches several tons, mainly supplied to pharmaceutical giants such as Pfizer and Novartis.
Application in Veterinary Medicine
Promote ovulation and increase pregnancy rate
In animal husbandry, improving the reproductive efficiency of animals is the key to increasing yield and economic benefits. It is widely used to promote ovulation in female animals and increase fertility rates. In the reproductive management of livestock such as cattle, pigs, and sheep, it can effectively stimulate ovarian activity, promote follicular development, and ovulation.
For example, in dairy farming, by using it reasonably, the estrus cycle of cows can be adjusted, allowing more cows to estrus at the appropriate time and facilitating artificial insemination (AI). Research has shown that after use, the ovulation rate of cows is significantly improved, and the pregnancy rate also increases. In pig farming, it can also be used to induce estrus and ovulation in sows, improve reproductive efficiency, and increase the number of piglets born.
Regulating the estrous cycle
Plays an important role in regulating the estrous cycle of animals. Through synchronous processing, a group of animals can enter estrus simultaneously, which is very beneficial for centralized breeding and improving reproductive management efficiency. In the breeding of livestock such as cattle and sheep, using ovalyse for estrus synchronization treatment can simplify the breeding plan and facilitate the arrangement of artificial insemination or embryo transfer operations.
For example, in dairy farming, the use of artificial insemination can make the cow population estrus at relatively concentrated times, which can improve the synchronization of conception and facilitate subsequent pregnancy management and calving arrangements. In sheep farming, estrus synchronization treatment can improve reproductive efficiency and increase the number of sheep herds.
Treating ovarian dysfunction
Ovarian dysfunction is one of the common problems that affect animal reproductive performance, such as ovarian cysts and anovulatory estrus. It can effectively treat these ovarian dysfunction diseases, restore normal ovarian function and reproductive ability in animals.
In dairy farming, ovarian cysts are one of the important causes of infertility in cows. The use of ovalyse can regulate hormone levels in cows, promote cyst regression, and restore normal ovulation function of the ovaries. Research has shown that after treatment with ovalyse, the pregnancy rate of cows with ovarian cysts is significantly improved and their reproductive performance is enhanced.
Improve the success rate of artificial insemination and embryo transfer
It also plays an important role in assisted reproductive technologies such as artificial insemination and embryo transfer. It can improve the ovulation quality of female animals, increase the number of available eggs, and provide better conditions for artificial insemination and embryo transfer.
During embryo transfer, the use of fertirelin acetate can synchronize the estrus cycles of donor and recipient animals, allowing embryos to implant and develop in a suitable uterine environment and improving the success rate of embryo transfer. At the same time, it can also improve luteal function, ensure sufficient progesterone secretion, and provide guarantees for the maintenance of pregnancy.
The synthesis of that belongs to the category of peptide synthesis, usually using solid-phase synthesis (SPPS) or liquid-phase synthesis. Starting from the basic principles of peptide synthesis and combining with the structural characteristics of ovalyse, this article provides a detailed introduction to its common synthesis methods.
In addition to solid-phase synthesis, it can also be synthesized through liquid-phase synthesis or fragment condensation methods.
1. Liquid phase synthesis method
The liquid-phase synthesis method is suitable for the synthesis of short peptides or complex peptides. For ovalyse, it can be divided into 2-3 fragments, synthesized separately in liquid phase, and then connected into complete peptides through condensation reaction. For example:
Fragment 1: Glp His Trp Ser Tyr;
Fragment 2: Gly Leu Arg Pro ethylamide;
Connect the two fragments using condensation reagents such as DCC/HOBt or HATU.
The advantage of liquid-phase synthesis method is that the reaction conditions are flexible, but it requires multiple purifications of intermediates and the operation is cumbersome.
2. Fragment condensation methodket
Fragment condensation method is a combination of solid-phase synthesis and liquid-phase synthesis. For example:
Synthesize longer fragments (such as Glp His Trp Ser Tyr) using solid-phase synthesis method;
Synthesize another fragment (such as Gly Leu Arg Pro ethylamide) using liquid-phase synthesis method;
Condense two fragments in the liquid phase.
Fragment condensation method can reduce the steps of solid-phase synthesis and improve synthesis efficiency, but it requires optimization of the conditions for fragment connection.
Selection and optimization of synthesis methods
The synthesis method of ovalyse needs to be selected and optimized based on the following factors:
Peptide length:
Short peptides (<10 amino acids) can be synthesized using liquid-phase synthesis method; It is recommended to use solid-phase synthesis for long peptides (>10 amino acids).
Complexity:
Peptides containing complex amino acids (such as Cys, Met) or modifying groups require solid-phase synthesis and optimized protection strategies.
Scale:
Solid phase synthesis method can be used for small-scale synthesis in the laboratory; Large scale industrial synthesis can consider liquid-phase synthesis or fragment condensation methods.
Cost:
The reagents and resins used in solid-phase synthesis are relatively expensive; The liquid-phase synthesis method has a lower cost, but requires more purification steps.
Synthesize instances and data
The following is an experimental data of solid-phase synthesis of ovalyse:
Resin:
Rink amide resin (0.25 mmol/g), 1 g;
Amino acid sequence:
Glp His (Trt) - Trp (Boc) - Ser (tBu) - Tyr (tBu) - Gly Leu Arg (Pbf) - Pro;
C-terminal:
Ethylamide;
Cutting reagent:
TFA/TIS/H ₂ O=95:2.5:2.5, 2 mL;
Cutting time:
2 hours;
Purification method:
HPLC (C18 column, acetonitrile/water+0.1% TFA);
Yield:
0.8 g of crude product (theoretical amount 1.213 g, yield 66%), 0.3 g of pure product (purity>95%);
Mass spectrometry identification:
MS (ESI) m/z: [M+H] ⁺ calculated value is 1214.37, measured value is 1214.40.
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