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Ganirelix acetate injection is a synthetic peptide with high antagonistic activity against naturally occurring GnRH. It competitively blocks GnRH receptors on pituitary gonadotropin cells and subsequent transduction pathways, resulting in a rapid and reversible inhibition of gonadotropin secretion.It has a significant effect and is commonly used in women undergoing controlled ovarian stimulation (COS) with assisted reproductive technology (ART), such as in vitro fertilization or artificial insemination techniques, to help women better induce ovulation and obtain more dominant oocytes.
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Ganirelix Acetate COA
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| Certificate of Analysis | ||
| Compound name | Ganirelix Acetate | |
| Grade | Pharmaceutical grade | |
| CAS No. | 123246-29-7 | |
| Quantity | 37g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090056 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.32% |
| Loss on drying | ≤1.0% | 0.14% |
| 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% | 99.90% |
| Single impurity | <0.8% | 0.27% |
| Total microbial count | ≤750cfu/g | 319 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 220ppm |
| Storage | Store in a sealed, dark, and dry place below2-8°C | |
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| Chemical Formula: | C80H112ClN17O13 |
| Exact Mass: | 1554 |
| Molecular Weight: | 1555 |
| m/z: | 1554 (100.0%), 1555 (86.5%), 1556 (37.0%), 1556 (32.0%), 1557 (27.7%), 1558 (11.8%), 1557 (10.4%), 1555 (6.3%), 1556 (5.4%), 1559 (3.1%), 1556 (2.7%), 1557 (2.3%), 1557 (2.3%), 1558 (2.2%), 1557 (2.0%), 1558 (1.7%), 1556 (1.1%) |
| Elemental Analysis: | C, 61.78; H, 7.26; Cl, 2.28; N, 15.31; O, 13.37 |

Ganirelix acetate injection is a synthetic peptide that belongs to the GnRH antagonist class. It has high antagonistic activity against naturally occurring GnRH and plays an important role in the medical field, especially in the treatment of female reproductive health-related diseases.
Applications related to assisted reproductive technology
(1) Preventing premature onset of LH peak in controlled ovarian stimulation (COS)
When receiving COS treatment, patients need to undergo controlled ovarian hyperstimulation with medication to obtain multiple mature ovums for assisted reproductive technologies such as in vitro fertilization (IVF). However, if LH peak appears too early during ovulation induction, it can lead to premature luteinization and ovulation of follicles, resulting in a decrease in the number and quality of ovums obtained, thereby affecting the success rate of assisted reproductive therapy.
Being able to competitively block GnRH receptors on pituitary gonadotropin cells, inhibit LH secretion, avoid premature LH peaks, ensure synchronous and full development of multiple follicles, and create conditions for obtaining high-quality ovums.
For example, in IVF technology, patients usually start using FSH for ovulation induction treatment on the second or third day of their menstrual cycle.

Based on the ovarian response, such as the number and size of growing and developing follicles, as well as the level of estradiol in the peripheral blood circulation, daily subcutaneous injection of acetic acid plus nifedipine (0.25mg) starting from the 5th or 6th day after FSH treatment can effectively prevent the occurrence of premature LH peaks.Due to its half-life, the time interval between two injections and the time interval between the last injection and hCG injection should not exceed 30 hours, otherwise premature LH peaks may occur.
If medication is taken in the morning, starting from the 5th or 6th day of FSH ovarian stimulation, administer acetic acid ganciclovir and continue the entire FSH treatment process until the day of ovulation induction (including the day of ovulation induction).If taking medication at night, start from the 5th day of ovarian stimulation and continue the entire FSH treatment process until the night before ovulation induction. The related study 38607 evaluated the safety and efficacy of acetic acid ganrelic in European women receiving controlled ovarian stimulation, using the Busherelin long regimen as a control group.

A total of 701 subjects were included in the intention to treat population (463 in the acetic acid group and 238 in the busherelin group). The main selection criteria are age 18-39 years old, body mass index between 18-29kg/m ², and menstrual cycle within the normal range of 24 to 35 days.The acetic acid ganrelic group started subcutaneous injection of acetic acid ganrelic (0.25mg/day) on the 6th day of FSH treatment until the day of receiving hCG (including that day);The Busherelin group started receiving treatment (0.6mg/day, administered via nasal route) from the 21st to the 24th day of the menstrual cycle.
After 14 days, if a decrease in regulation (E2 ≤ 50pg/mL) was reached, FSH treatment was initiated until the day of hCG treatment. The main efficacy indicator is the number of oocytes obtained on the day of ovum retrieval. Calculated per initiation cycle, the average number of oocytes obtained by subjects in the acetic acid garenicol group was 8.7, while that in the busherelin group was 9.7. The lower limit of the 97.5% confidence interval for the difference was -1.8. The results of this study and other similar studies indicate that acetic acid garenicol is significantly effective in preventing LH peaks.
Information source: Baidu Baike entry for "Acetic Acid Ganirek Injection"
(2) Reduce the occurrence of ovarian hyperstimulation syndrome (OHSS)
Ovarian hyperstimulation syndrome is one of the common complications in assisted reproductive technology, mainly manifested as ovarian enlargement, ascites, pleural effusion, blood concentration, electrolyte imbalance, etc. In severe cases, ganirelix acetate injection can be life-threatening. The use of ovulation inducing drugs is one of the important causes of OHSS, as these drugs stimulate the ovaries, causing multiple follicles to develop simultaneously, resulting in increased ovarian volume and elevated estrogen levels.
By regulating hormne levels in the body, the stimulation of the ovaries by ovulation inducing drugs can be reduced, thereby lowering the risk of OHSS. Continuing to use acetic acid garenicol after ovum retrieval can further reduce ovarian stimulation response and help patients recover. For example, clinical trials have shown that compared to the use of GnRH agonists, their use can reduce the incidence of OHSS, decrease patient discomfort and complications caused by OHSS, and improve the safety and comfort of treatment.

(3) Improve the success rate of assisted reproductive therapy
Taking into account the above effects, the success rate of treatment can be significantly improved in assisted reproductive technology.
By preventing premature LH peak, promoting ovulation, improving ovum quality, and reducing OHSS, favorable conditions have been created for obtaining high-quality ovums and embryos, increasing the chances of conception. At the same time, the treatment process has been optimized, the occurrence of complications has been reduced, and the patient's treatment experience and compliance have been improved.
Information source: Baidu Baike entry for "Acetic Acid Ganirek Injection"
Treatment of endometriosis
LH may play a certain role in the occurrence and development of endometriosis. Excessive LH levels may stimulate the growth and proliferation of ectopic endometrial tissue, exacerbating the condition. As a GnRH antagonist, it can inhibit the secretion of LH, thereby regulating hormne levels in the body, reducing the stimulation of ectopic endometrial tissue, and relieving patients' symptoms.


For example, for endometriosis patients with mild to moderate dysmenorrhea who wish to preserve fertility, treatment with it can downregulate endogenous hormne levels, reduce estrogen production, decrease the proliferation rate of endometrial cells and the probability of new blood vessel formation, thereby relieving pain and controlling disease progression. However, there is currently relatively little research on its treatment of endometriosis, and further clinical studies are needed to confirm its exact efficacy and safety.
Source of information:
39 Health Network "What is the function of Qingle Acetic Acid Gani"
39 What diseases can be treated with acetic acid injection of Ganiric acid
Clinical data research
Study 38607 evaluated the safety and efficacy of ganirelix acetate injection in European women receiving controlled ovarian stimulation, using the Busherelin Long Plan as a control group. A total of 701 subjects were included in the intention to treat population (463 in the local group and 238 in the busherelin group). The main selection criteria are age 18-39 years old, body mass index between 18-29kg/m2, and menstrual cycle within the normal range of 24 to 35 days. This product group started subcutaneous injection of this product (0.25mg/day) on the 6th day of FSH treatment until the day of receiving hCG (including that day).
The Busherelin group started receiving treatment (0.6mg/day, administered via nasal route) from the 21st to the 24th day of the menstrual cycle. After 14 days, if a decrease in regulation (E2 ≤ 50pg/mL) was reached, FSH treatment was initiated until the day of hCG treatment. The main efficacy indicator is the number of oocytes obtained on the day of egg retrieval. Calculated based on each start-up cycle, the average number of oocytes obtained by the subjects in this group was 8.7, while that in the Busherelin group was 9.7. The lower limit of the 97.5% confidence interval for the difference was -1.8.
Study 103001 evaluated the safety and efficacy of leuprorelin in North American women receiving controlled ovarian stimulation, using the leuprorelin regimen as a control group. A total of 297 subjects were included in the intention to treat population (198 in the product group and 99 in the leuprorelin group). The main selection criteria are the same as study 38607. This product group started subcutaneous injection of this product (0.25mg/day) on the 6th day of FSH treatment until the day of receiving hCG (including that day).

The leuprorelin group started receiving subcutaneous injections (1.0mg/day) from the 21st to the 24th day of the menstrual cycle. After 14 days, if a decrease in regulation (E2 ≤ 50pg/mL) was reached, FSH treatment was initiated until the day of hCG treatment. The main efficacy indicator is the number of oocytes obtained on the day of egg retrieval. Calculated based on each start-up cycle, the average number of oocytes obtained by the subjects in this product group was 11.1, while that of leuprorelin was 13.5. The lower limit of the 97.5% confidence interval for the difference was -4.0.

I. Solid-Phase Peptide Chain Assembly
Ganirelix acetate is a decapeptide GnRH antagonist. The industrial production adopts the Fmoc solid-phase synthetic route with Rink Amide resin as the solid support.
Each chirally modified amino acid is sequentially coupled starting from C-terminal D-Ala toward the N-terminus, and homoarginine is protected via diethyl side-chain modification.
DIC/HOBt is used as the coupling reagent. Fmoc deprotection is performed with piperidine at each step, the ninhydrin test is applied to verify the coupling endpoint, and unreacted amino groups are capped with acetic anhydride.
After the assembly of the full peptide chain, N-terminal acetylation is carried out with acetic anhydride to obtain fully protected peptide resin.
II. Cleavage and Crude Peptide Preparation
A mixed TFA cleavage cocktail supplemented with scavengers is used to cleave the peptide-resin linkage and remove all side-chain protecting groups. The cleavage solution is poured into cold methyl tert-butyl ether to precipitate crude peptide. Multiple rounds of centrifugation and washing are conducted to remove hydrophobic byproducts, followed by vacuum drying to yield crude peptide.
III. Purification, Salt Formation and Pre-Formulation Treatment
The crude peptide is purified by gradient elution on C18 reversed-phase HPLC to separate epimers and deletion peptide impurities. The main peak fraction is collected, desalted, and quantitatively salt-formed with acetic acid, then lyophilized to obtain high-purity ganirelix acetate API.
The API is dissolved in sterile water, subjected to sterile filtration, filled and sealed to produce the injection. This process features safe operation and controllable impurities. The purity of the API can exceed 99% with an overall yield of approximately 30%, making it suitable for large-scale manufacturing of injectable raw materials.
FAQ
It is used as a fertility medicine to prevent premature LH surges or ovulation in women undergoing fertility treatment of controlled ovarian hyperstimulation. It may also help reduce the need for FSH, which is also needed for ovulation.
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