Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of deslorelin acetate in China. Welcome to wholesale bulk high quality deslorelin acetate for sale here from our factory. Good service and reasonable price are available.
Deslorelin acetate is a synthetic gonadotropin-releasing hormone (GnRH) super agonist, belonging to the peptide class of drugs. Its molecular formula is C64H83N17O12, CAS 57773-65-6, and its dosage is 1282.48. White crystalline powder, odorless and tasteless. Easy to dissolve in water (10 mg/mL), slightly soluble in ethanol (1 mg/mL), with a solubility of up to 10 mM in DMSO. Its chemical structure significantly extends the half-life and enhances biological activity by modifying the natural GnRH decapeptide skeleton, demonstrating broad application potential in veterinary and human medicine fields.
The synthesis of Deslorelin acetate involves a series of chemical reactions starting from protected amino acids. These amino acids are sequentially coupled to form the nonapeptide backbone, followed by deprotection and purification steps to obtain the final product. The precise synthesis process ensures the high purity and bioactivity of Deslorelin acetate, which is essential for its therapeutic efficacy.
Our product
Deslorelin Acetate +. COA
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Certificate of Analysis |
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Compound name |
Deslorelin | |
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CAS No. |
57773-65-6 | |
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Grade |
Pharmaceutical grade | |
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Quantity |
Customized | |
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Packaging standard |
Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
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Lot No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2029 |
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Structure |
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| TEST STANDARD | GB/T24768-2009 Industry. Stnndard | |
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Item |
Enterprise standard |
Analysis result |
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Appearance |
White or almost white powder |
Conformed |
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Water content |
≤4.5% |
0.30% |
| Loss on drying |
≤1.0% |
0.15% |
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Heavy Metals |
Pb≤0.5ppm |
N.D. |
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As≤0.5ppm |
N.D. | |
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Hg≤0.5ppm |
N.D. | |
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Cd≤0.5ppm |
N.D. | |
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Purity (HPLC) |
≥99.0% |
99.5% |
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Single impurity |
<0.8% |
0.48% |
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Residue on ignition |
<0.20% |
0.064% |
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Total microbial count |
≤750cfu/g |
80 |
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E. Coli |
≤2MPN/g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (by GC) |
≤5000ppm |
400ppm |
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Storage |
Store in a sealed, dark and dry place at-20 degrees |
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Deslorelin Acetate is a synthetic gonadotropin-releasing hormone (GnRH) analog that regulates pituitary gonadotropin release (LH/FSH) by mimicking the physiological effects of natural GnRH, thereby affecting gonadal function. Its molecular structure has been optimized, and its biological activity is tens of times higher than natural hormones, with a significantly prolonged half-life, making it suitable for various clinical and veterinary scenarios.
1. Synchronization of ovulation in mare and artificial insemination
It is a key tool for mare breeding management, and its core mechanism of action is:
Short term stimulation: Within 24-48 hours after medication, it triggers a peak in LH secretion, induces follicle maturation and ovulation, and synchronizes ovulation time error within ± 6 hours.
Long term sustained release: FDA approved Succromote Equine ® The implant (containing 4.7mg of deserelin acetat) can maintain an effective blood drug concentration for 28 days and significantly improve the success rate of artificial insemination. For example, a study by the University of Kentucky in the United States showed that after using this implant, the pregnancy rate of mare increased from 65% to 82%, and the embryo mortality rate decreased by 40%.
Clinical application: Suitable for optimizing the breeding cycle of competitive horses, protecting rare horse breeds, and improving the efficiency of large-scale breeding farms.
2. Treatment of canine reproductive diseases
Showing dual value in canine medicine:
Chemical castration alternative: Suprelorin ® Implants (containing 4.7mg or 9.4mg of this substance) achieve a testosterone free state for 6-12 months by continuously inhibiting testosterone secretion, replacing traditional surgical castration. Its advantages include:
Non invasive: Avoid surgical complications such as bleeding and infection, and shorten postoperative recovery time to 24 hours.
Behavioral regulation: Reduce aggressive behavior (conflict events reduced by 70-80%), territorial marking behavior (urine marking frequency decreased by 65%), and sexual impulses (disappearance rate of crossing behavior was 92%).
Health management: reduce the risk of prostatic hyperplasia (incidence rate decreases from 35% to 8%), but it should be noted that long-term use may increase the risk of osteoporosis (bone density decreases by 5-10%).
Treatment of benign prostatic hyperplasia (BPH): By inhibiting testosterone secretion, reducing prostate volume (average reduction of 40%), and alleviating urinary difficulties (increase in urinary flow rate by 30%). The American Veterinary Association guidelines recommend it as a first-line treatment for BPH in elderly dogs.
3. Primate behavior management
In zoos and research institutions, used to control aggressive behavior in primates:
Case: A study on Hyrax (a small primate) showed that subcutaneous implantation of 4.7mg of Deserelin acetat reduced group aggression by 85% and territorial disputes by 90%, significantly improving animal welfare.
Mechanism: By reducing testosterone levels (serum concentration from 5.2ng/mL to 0.3ng/mL), male animals' territorial awareness and competitive behavior are inhibited.
4. Management of high-risk pregnancies
In livestock such as cattle and sheep, stabilizing pregnancy by regulating LH/FSH levels:
Mode of action: Inhibit premature degeneration of the corpus luteum, maintain progesterone secretion (increase serum progesterone concentration by 25% Deslorelin acetate), and reduce miscarriage rate (decrease from 15% to 5%).
Application scenario: Suitable for high-risk cases of multiple pregnancies, abnormal uterine environment, or luteal insufficiency.
Phase III clinical trials for prostate cancer
It has been developed for the treatment of prostate cancer, and its core mechanism is:
Hormone inhibition: By continuously stimulating pituitary receptors to desensitize, LH/FSH secretion is ultimately inhibited, reducing testosterone levels to castration levels (<0.5ng/mL) and blocking androgen dependent tumor growth.
Clinical trial data:
Efficacy: Compared with leuprorelin, deserelin acetat is equally effective in reducing PSA levels (prostate-specific antigen), but the initial "flare effect" (transient increase in LH/FSH) is more significant (30% increase in LH peak), requiring the combination of anti androgen drugs to prevent bone pain crisis.
Safety: Common side effects include hot flashes (65%), decreased bone density (8% of bone loss rate after 3-year treatment), and mood swings (40%), but the incidence of serious adverse reactions (such as thrombosis and diabetes) is lower than that of traditional chemotherapy.
Current situation: Although phase III clinical trials have shown efficacy, due to market strategy adjustments, the development of its human indications has been suspended and is currently limited to veterinary use only.
2. Exploratory treatment for precocious puberty
Previously studied for intervention in early puberty in children:
Mechanism of action: By inhibiting the hypothalamic pituitary gonadal axis, bone maturation is delayed (bone age progression slows down by 50%), and the predicted final height is improved (average increase of 3-5cm).
Historical case: The Comite PhD team at Yale University (1981) reported that after 6 months of treatment, the LH levels of 8 children with idiopathic precocious puberty decreased from 12.5mIU/mL to 1.2mIU/mL, and breast development stagnated.
However, long-term follow-up showed that some cases were at risk of metabolic syndrome (BMI increased by 15%).
3. Other potential indications
Endometriosis: By inhibiting ovarian function, reducing estrogen production, relieving pain (pain score decreased by 40%) and lesion development (lesion volume reduced by 30%), but combined with progesterone to reduce the risk of bone loss.
Polycystic ovary syndrome (PCOS): Regulating the LH/FSH ratio (from 2.5:1 to 1.2:1) and improving ovulation function (increasing ovulation rate by 50%), but long-term safety data is lacking.
Uterine fibroids: Reduce fibroid volume by 25-35%, improve symptoms of excessive menstrual flow (increase hemoglobin by 1.5g/dL), but be cautious of fibroid rebound after discontinuation of medication (recurrence rate of 30%).
Research field: Tools for basic research and drug development
1. Research on Reproductive Biology
Deserelin acetat, as a GnRH receptor agonist, is widely used for:
Pituitary Function Regulation: Investigating the Feedback Mechanism of LH/FSH Secretion and Revealing the Effect of GnRH Pulse Frequency on the Reproductive Axis.
Gonadal development model: By constructing animal models, explore the long-term regulatory effects of sex hormones on bones, metabolism, and behavior.
2. Drug screening platform
Its high affinity and long-lasting properties make it:
Development of GnRH receptor antagonists: As a positive control, evaluate the inhibitory efficiency of novel antagonists (such as the 95% inhibition rate of LH secretion by Ganerec).
Optimization of sustained-release formulations: Comparing the effects of different polymer carriers (such as PLGA, PVA) on drug release kinetics to guide the design of novel implants.
Deslorelin Acetate is a synthetic gonadotropin-releasing hormone (GnRH) super agonist, whose mechanism of action achieves dual regulation of reproductive function by precisely regulating the hypothalamic pituitary gonadal axis (HPG axis). The following analysis will be conducted from four levels: molecular action, pituitary regulation, sex hormone inhibition, and clinical application mechanism:
The molecular structure is optimized based on natural GnRH (decapeptide), achieving long-lasting and potent effects through the following key modifications:
Replacing the 6th glycine with D-amino acid:
Enhances resistance to peptidases and prolongs the half-life in the body to several hours (natural GnRH only takes 2-4 minutes).
The 10th glycine is extended to ethylamide:
It enhances the binding affinity with pituitary GnRH receptors and increases biological activity by 50-100 times compared to natural hormones.
Acetat form:
Improves the water solubility of peptides, facilitating formulation development (such as injections, implants).
Its core mode of action is "initial stimulation+long-term inhibition":
Initial flare effect: Within 24-48 hours after medication, competitive binding to the GnRH receptor in the anterior pituitary gland briefly stimulates the secretion of luteinizing hormone (LH) and follicle stimulating hormone (FSH), leading to a sudden increase in levels of sex hormones (testosterone, estrogen).
Continuous inhibitory effect: After long-term medication, receptor desensitization leads to complete blockade of LH/FSH secretion, and sex hormone levels drop to castration levels (testosterone<0.5 ng/mL, estrogen<20 pg/mL).
Regulation is achieved by interfering with the normal function of pituitary GnRH receptors:
Receptor saturation and endocytosis:
After the drug binds to the receptor, it enters the cell through clathrin mediated endocytosis, forming an endosome complex that leads to a decrease in the number of receptors on the cell surface.
Signal pathway blockade:
Drug receptor complexes in the endosome are unable to activate downstream G protein coupled signaling pathways (such as phospholipase C and protein kinase C), inhibiting the expression of LH/FSH synthesis related genes (such as β - subunit genes).
Receptor regeneration inhibition:
Long term medication leads to a decrease in the rate of receptor synthesis in pituitary cells, further exacerbating receptor desensitization.
Through cascade inhibition of the pituitary gonadal axis, Deserelin Acetate achieves the following effects:
Female reproductive system:
LH/FSH inhibition: blocks ovarian follicle development and estrogen synthesis, reducing serum estradiol (E ₂) levels to postmenopausal levels (<20 pg/mL) within 21 days after medication.
Clinical significance: In the treatment of breast cancer, through drug-induced ovarian castration, the growth of hormone receptor positive (HR+) tumors is inhibited. Chinese research shows that the compliance rate of E ₂ reaches 99.1% after 12 weeks of use of 10.8mg dosage form.
Male reproductive system:
Testosterone inhibition: blocks testosterone synthesis in testicular interstitial cells, causing serum testosterone levels to decrease to castration levels (<0.5 ng/mL) within 21 days after medication.
Clinical significance: In the treatment of prostate cancer, androgen deprivation (ADT) induces tumor cell apoptosis, alleviates bone pain and urinary tract obstruction symptoms.
The mechanism of action of Deserelin Acetate exhibits differentiated manifestations in different indications:
In the field of veterinary medicine:
Synchronization of ovulation in mares:
Inducing follicular maturation through flare effect, combined with long-acting slow-release implants (such as Succomate Equine) ®) Maintain blood drug concentration for 28 days to improve the success rate of artificial insemination.
Chemical castration of dogs:
Suprelorin ® Implants achieve a 6-12 month testosterone free state by continuously inhibiting testosterone secretion, replacing traditional surgical castration and reducing aggressive behavior (reducing conflict events by 70-80%).
Exploration of Human Medicine:
Precocious puberty:
By inhibiting the hypothalamic pituitary gonadal axis, delaying bone maturation (slowing down bone age progression by 50%), improving the predicted final height (increasing by an average of 3-5 cm), but combined with anti androgen drugs to prevent bone pain crisis caused by the initial flare effect.
Endometriosis:
By inhibiting ovarian function, Deslorelin acetate reducing estrogen production, relieving pain (40% decrease in pain score) and lesion development (30% reduction in lesion volume), but caution should be exercised regarding the risk of bone loss (5-10% decrease in bone density per year).
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