Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of fertirelin acetate in China. Welcome to wholesale bulk high quality fertirelin acetate for sale here from our factory. Good service and reasonable price are available.
Fertirelin acetate is a pharmaceutically modified derivative of raw fertirelin peptide conjugated with ethanoate salt groups. Its most prominent key characteristic lies in the unique structural advantage brought about by gentle ethanoate molecular modification, which effectively solves the prominent problems of poor water solubility and low systemic bioavailability of unmodified native fertirelin raw peptide. Its accurate molecular formula is C₅₅H₇₆N₁₆O₁₂ and precise molecular weight is 1153.29 under standard testing conditions.
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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 | 15g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202612090051 | |
| MFG | Dec 9th 2026 | |
| EXP | Dec 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.72% |
| Loss on drying | ≤1.0% | 0.51% |
| 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% | 0.27% |
| Total microbial count | ≤750cfu/g | 93 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 347ppm |
| Storage | Store in a sealed, dark, and dry place below -15°C | |
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| Chemical Formula | C57H80N16O14 | |
| Exact Mass | 1212.6 | |
| Molecular Weight | 1213.37 | |
| m/z | 1212.60(100.0%), 1213.61(61.6%), 1214.61(18.7%), 1153.58(5.9%), 1154.58(3.5%), 1155.59(2.5%), 1154.59(2.5%), 1155.59(1.5%), 1155.59(1.0%) | |
| Elemental Analysis | C,56.42; H,6.65; N,18.47; O,18.46 | |
As a synthetic polypeptide hormonal veterinary and human drug, its fixed peptide sequence remains pGlu-HWSYGLRP-NHEt. The chemical introduction of ethanoate counterions does not alter or weaken its inherent core pharmacological biological activity. It still exerts therapeutic effects by specifically binding to targeted gonadoliberin receptors distributed in the anterior pituitary gland to precisely regulate the secretion balance of the hypothalamic–pituitary–gonadal axis: it generates mild transient stimulation at the initial administration stage and triggers sustained long-term inhibition of luteinizing hormone (LH) .
Reduction of Superovulatory Response
Superovulatory response is a common adverse reaction in reproductive regulation, especially in animal breeding and assisted reproductive technology (ART) in humans. It is mainly characterized by excessive ovulatory event, which may lead to complications such as multiple pregnancy and ovarian hyperstimulation syndrome (OHSS). Such conditions not only reduce breeding quality but may also endanger maternal health in severe cases.Benefiting from the high pharmacological activity conferred by ethanoate modification, fertirelin acetate can precisely suppress excessive ovulatory event at high doses, making it a key drug in scenarios requiring accurate control of ovulatory event count. Its application is mainly concentrated in animal breeding, while it also has potential adaptability in human assisted reproduction.
Mechanism of Action: Precise ovulatory event Regulation Based on Acetate Modification
As a synthetic therapeutic gonadoliberin analog, this pharmaceutical product carries the fixed active polypeptide sequence pGlu-HWSYGLRP-NHEt.The chemical introduction of the ethanoate counterion moiety does not interfere with or alter its inherent core pharmacological activity, but significantly strengthens its specific binding affinity to pituitary gonadoliberin receptors and effectively prolongs its sustained duration of physiological action inside animal bodies. The core molecular mechanism underlying the strong inhibition of excessive superovulatory response is its unique biphasic bidirectional regulatory effect:
At low doses, it transiently stimulates the pituitary to secrete luteinizing hormone (LH) and follicle‑stimulating hormone (FSH), promoting normal follicular development and ovulatory event.
At high doses with continuous administration, it downregulates the sensitivity of pituitary gonadoliberin receptors via negative feedback, reducing excessive secretion of LH and FSH, thereby inhibiting the development and ovulatory event of superfluous follicles and achieving precise control of ovulatory event number.
Compared with other gonadoliberin analogs without ethanoate modification, the product shows distinct advantages:
Acetate modification improves water solubility, enabling rapid absorption after injection, prompt achievement of effective plasma concentrations, and timely suppression of excessive ovulation.
Enhanced stability prolongs its in vivo duration, maintaining stable regulatory effects without frequent dosing, lowering the risk of uncontrolled ovulatory event due to delayed administration, and ensuring precise regulation.
Main Application Scenario: Precise Breeding Regulation in Animal Production
At present, the use of the product to reduce superovulatory response is mainly concentrated in veterinary medicine, especially in large‑scale breeding of cattle, sheep and other livestock.In intensive farming, superovulation techniques are commonly used to improve reproductive efficiency. However, excessive ovulatory event easily leads to multiple pregnancy:
- Multiple pregnancy in cows increases the risk of dystocia and postpartum care difficulties, reduces calf survival rate, and may cause ovarian damage.
- Multiple pregnancy in ewes can result in fetal growth retardation, insufficient postpartum lactation, and other problems, causing substantial economic losses.
The product effectively addresses this problem through its precise ovulation‑inhibiting effect.In practice, after superovulation treatment, farmers administer an appropriate (usually high) dose of fertirelin acetate according to the livestock species, body weight and reproductive status. It suppresses further development and ovulatory event of excess follicles, limiting ovulatory event to a reasonable range (e.g., 1–2 ovulations per time in cows). This ensures reproductive efficiency while avoiding complications associated with multiple pregnancy.Meanwhile, the ease of administration afforded by ethanoate modification makes it suitable for large‑scale use. It can be quickly delivered via subcutaneous or intramuscular injection.
In addition, the product also functions by reducing superovulatory responses in the adjunctive treatment of animal reproductive disorders. For example, in cows with follicular cysts, which present with ovulatory disorders and excessive estrus, high‑dose this ethanoate inhibits superovulation, regulates the hypothalamic‑pituitary‑gonadal axis, promotes cyst regression, and helps restore normal estrous and ovulatory cycles, further improving breeding quality.Relevant studies show that intervention with high‑dose it reduces the incidence of superovulatory response in livestock by more than 60%.
Application Advantages and Precautions
Its main advantages are:
High precision: ovulatory event number can be controlled by adjusting the dose to meet the breeding requirements of different livestock.
High safety: ethanoate modification results in mild metabolism in vivo, low risk of cumulative toxicity, minimal damage to the maternal reproductive system, and rapid recovery of reproductive function after drug withdrawal.
Precautions:
Dose and timing must be strictly controlled;
Too low a dose fails to achieve effective inhibition;
Too high a dose may excessively suppress ovulation, leading to delayed or anovulation.
Administration is usually performed 24–48 hours after superovulation, synchronized with the estrous cycle, for optimal inhibitory effect.
Doses should be flexibly adjusted according to species, body weight, reproductive status and individual differences to avoid blind use.
Adjuvant Treatment for Human Fertility (Potential Application)
Although the product is currently approved mainly for veterinary use, as a gonadoliberin analog, its core pharmacological activity is highly similar to commonly used gonadoliberin‑based fertility drugs in human clinics (such as triptorelin ethanoate). Moreover, the advantages in bioavailability brought about by acetate modification give it potential value in assisted human reproductive therapy.Preliminary studies have shown that the drug can stimulate follicular growth in women, especially when combined with drugs such as estradiol benzoate. However, its human application is not yet widespread and remains in the early research and clinical validation stage.
Potential Mechanism: Precise Stimulation and Regulation of Follicular Growth
In human fertility treatment, poor follicular development and ovulatory disorders are major causes of infertility. Clinically, gonadoliberin drugs are often used to stimulate follicular growth and ovulation to facilitate conception.The potential mechanism of fertirelin acetate in adjuvant human fertility treatment is closely related to its stimulatory effect at medium and low doses:After administration at medium or low doses, this ethanoate binds to human pituitary gonadoliberin receptors and stimulates the secretion of LH and FSH - key hormones for follicular development and maturation.
FSH stimulates the proliferation of follicular granulosa cells and promotes follicular fluid secretion, driving follicular maturation.LH promotes follicular rupture and completes ovulation.Compared with conventional gonadoliberin analogs in human clinics, the product has potential advantages due to acetate modification:Higher water solubility and bioavailability, enabling rapid absorption and faster follicular stimulation, shortening the developmental cycle.
Longer duration of action, maintaining stable plasma concentrations and avoiding uneven follicular growth or abnormal ovulation caused by fluctuating drug levels.
Synergistic enhancement of follicular growth when combined with estradiol benzoate:
Estradiol benzoate supplements estrogen to provide a favorable endocrine environment for folliculogenesis. Together with the product, it significantly improves follicular maturation and ovulation rates, laying a foundation for conception.
Early Research Progress and Application Limitations
In early exploratory clinical studies, researchers administered medium‑to‑low‑dose subcutaneous the product to infertile patients with ovulatory disorders, with some also receiving estradiol benzoate.Results showed significant improvement in follicular development, increased maturation and ovulation rates, and no obvious adverse reactions, preliminarily confirming the feasibility of its use in adjuvant human fertility treatment.In addition, its ease of administration supports potential clinical translation: subcutaneous injection without complex devices allows self‑administration under medical guidance, greatly improving convenience.
However, multiple limitations currently restrict its widespread use in human fertility therapy:Clinical studies are still in the early stage, with small sample sizes and short durations. Large‑scale, long‑term data are needed to confirm effects on conception rate, pregnancy outcomes, and long‑term safety.Dosage regimens are not fully standardized. Optimal dose, timing, and combination ratios with other drugs require further study and optimization based on individual patient differences (age, ovarian function, cause of infertility, etc.).The metabolic profile and dose–response relationship in humans require further clarification to prevent OHSS and ensure safety.
Several mature gonadoliberin analogs (e.g., triptorelin acetate, leuprorelin acetate) are already widely used clinically. It must establish unique advantages to break through existing application barriers.
Future Application Prospects
With the rising incidence of human infertility and growing demand for assisted reproductive technologies, the future of the product as a potentially advantageous gonadoliberin analog is promising.Future directions include:Conducting large‑scale, long‑term clinical trials to establish standardized, safe and effective dosing regimens and optimize combinations with other fertility agents.
Leveraging acetate modification to develop advanced dosage forms, such as long‑acting injections, to reduce dosing frequency and improve patient compliance.Optimizing delivery methods to enhance targeting and minimize systemic endocrine effects, further improving safety.Integrating precision medicine to design personalized regimens based on genetic characteristics, ovarian function and individual differences, enabling precise regulation of follicular growth and improving the success rate of assisted reproduction.
references
LH and FSH response of Holstein heifers to fertiralin acetate, gonadorelin and buserelin, 1990
Influence of gonadoliberin analogue (fertirelin-acetate) doses on synchronization of ovulatory event and fixed-time artificial insemination in lactating dairy cows, 2002
Optimum Dose of LH-RH Analogue Fertirelin Acetate for the Induction of ovulatory event in Mice, 2005
FAQ
Q1: What class of compound is fertiralin acetate?
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A1: It is a synthetic GnRH (gonadotropin-releasing hormone) peptide agonist mainly applied in veterinary reproduction.
Q2: What core function does fertirelin acetate perform in livestock breeding?
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A2: It stimulates pituitary secretion of LH and FSH to induce ovulation, synchronize estrus and raise conception rates for dairy cows and cattle.
Q3: What is the proper long-term storage condition for fertiralin acetate raw powder?
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A3: Fertirelin acetate pharmaceutical raw powder requires complete airtight sealing with moisture-proof aluminum foil packaging before storage. It should be placed in a constant-temperature freezer maintained at -20°C within a light-shielded, dry, low-humidity storage space. Long-term exposure to ambient light, elevated temperature or humid air will disrupt the intact peptide molecular chain, accelerate chemical decomposition and cause irreversible degradation of the active ingredient. Such improper storage will drastically reduce product purity, weaken its original reproductive regulatory biological activity, and render the raw material ineffective for subsequent veterinary preparation production and clinical breeding applications.
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