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Deslorelin, usually in the form of an implant, is a solid implant that is white or slightly yellowish in color. Its shape may vary depending on the manufacturer, but deslorin is usually cylindrical or rod-shaped. Molecular formula C64H83N17O12, CAS 57773-65-6, is a gonadotropin-releasing hormon (GnRH) analogue. The solubility in water is low because it is designed for slow release to continuously release drugs in animal bodies, thereby maintaining effective concentration. Relatively stable at room temperature, but needs to be stored away from light to prevent drug degradation. In addition, as it is designed for implantation in animals, it usually has good resistance to biodegradation. As an implant, Deserellin needs to have a certain mechanical strength so that it will not break or dissolve when implanted in animals. It should have a certain degree of hardness and toughness to withstand the mechanical stress during the implantation process. Mainly used for reproductive control of animals, especially horses. It is widely used in the veterinary field to inhibit animal estrus and ovulation by inhibiting the secretion of gonadotropins.
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Customized Bottle Caps And Corks:
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Chemical Formula |
C64H83N17O12 |
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Exact Mass |
1282 |
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Molecular Weight |
1282 |
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m/z |
1282 (100.0%), 1283 (69.2%), 1284 (23.6%), 1283 (6.3%), 1285 (5.3%), 1284 (4.3%), 1284 (2.5%), 1285 (1.7%), 1285 (1.4%) |
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Elemental Analysis |
C, 59.94; H, 6.52; N, 18.57; O, 14.97 |
Deslorelin, also known as Desloreli Acetate, is a synthetic gonadotropin-releasing hormon (GnRH) super agonist with a CAS number of 57773-65-6. As a peptide drug, it activates the GnRH receptor in the anterior pituitary gland by mimicking the action of natural GnRH, triggering the initial release of luteinizing hormon (LH) and follicle stimulating hormon (FSH). Subsequently, due to receptor desensitization, hormon levels are downregulated, ultimately inhibiting steroid synthesis in the ovaries and testes.
1. Mare breeding management
It is a key drug in the artificial insemination process of mare. By injecting Deserelin, the ovulation time of the mare can be precisely controlled, improving the fertility rate. Its mechanism of action is to stimulate LH secretion peak in the initial stage, promote follicle maturation and ovulation; Continuous administration inhibits LH and FSH secretion, avoiding unexpected ovulation. For example, Succomate Equine, approved by the US FDA, has been widely used in horse racing breeding, significantly shortening the breeding cycle.
2. Stable high-risk pregnancy
In livestock farming such as cattle and sheep, it can be used to stabilize high-risk pregnancies. By regulating hormon levels, the risk of miscarriage can be reduced. Research has shown that using Deserelin on female animals with a history of miscarriage increases pregnancy success rates by approximately 20%.
3. Alternative options for partner animal sterilization
Deserelin implants (such as Suprelorin) provide a non-surgical method of sterilization for dogs and ferrets. The implant slowly releases medication, continuously inhibits hormon secretion, and achieves chemical sterilization effect. Its advantage lies in reversibility: after discontinuation, reproductive function can be restored, making it suitable for pets that need to preserve their fertility.
4. Treatment of canine prostate hyperplasia
By inhibiting testosterone secretion, the prostate volume of dogs with benign prostatic hyperplasia (BPH) can be reduced, and urinary difficulties can be alleviated. Clinical data shows that after 3 months of treatment, the prostate volume decreased by an average of 35% and symptoms improved significantly.
1. Prostate cancer treatment
Deserelin, as a GnRH agonist, blocks the growth dependence of prostate cancer cells by continuously inhibiting testosterone secretion. Its long-acting formulation (such as monthly injection) can significantly reduce patients' serum testosterone levels to below castration levels. Although currently mainly used in animals, phase III clinical trials of human prostate cancer have shown that its efficacy is comparable to traditional castration surgery, and its side effects are more controllable.
2. Endometriosis and uterine fibroids
By inhibiting estrogen secretion, relieving the pain symptoms of endometriosis and reducing the volume of uterine fibroids. In clinical trials, patients' pain scores decreased by more than 50%, and the volume of fibroids decreased by about 40%.
However, long-term use may lead to side effects such as osteoporosis, and is currently mostly used as preoperative adjuvant therapy or short-term medication.
3. Intervention for precocious puberty
It can be used to treat central precocious puberty by inhibiting premature secretion of sex hormons, delaying bone maturation, and improving final height. Research shows that after 2 years of treatment, children are predicted to increase their adult height by 3-5cm.
4. Polycystic ovary syndrome (PCOS) management
By regulating LH secretion, correcting hyperandrogenism in PCOS patients and restoring ovulation cycle. Small scale clinical trials have shown that the ovulation recovery rate can reach 70% when combined with other drugs.
1. Reproductive Biology Research
As a specific agonist of GnRH receptor, Deslorelin is widely used to study the regulatory mechanism of hypothalamic pituitary gonadal axis. For example, through the Deserelin stimulation experiment, the secretion kinetics of LH and FSH can be accurately measured, providing a tool for reproductive endocrine disease models.
2. Drug development reference standards
And its analogues (such as goserelin) are used as standards for activity comparison and quality control in new drug development. Its high-purity formulation (such as the product corresponding to CAS number 57773-65-6) needs to undergo strict testing by HPLC, MS, etc. to ensure batch stability.
3. Research on Animal Behavior
In non-human primate research, it is used to explore the effects of sex hormons on social behavior, aggression, and other factors. For example, research on Rock Hyrax has found that the implantation of Deserelin can significantly reduce intra group aggressive behavior, providing a reference for understanding human social behavior.
Enzymatic synthesis is a method of synthesizing target compounds using enzymes as catalysts. In the process of enzymatic synthesis of desloreli, specific enzymes are used to catalyze a series of chemical reactions, thereby generating deserellin in an efficient, specific, and controllable manner. Although the specific enzymatic synthesis routes may vary depending on research and development, the following is a simplified description of the steps and chemical equations for enzymatic synthesis of Deserellin.
- The steps for enzymatic synthesis of Deserellin
Preparation of starting materials: Firstly, it is necessary to prepare starting materials suitable for enzymatic reactions. These raw materials typically have specific functional groups that can be recognized by enzymes and catalyze their conversion.
Select appropriate enzymes: Based on the structural characteristics of the starting material and target compound, select enzymes that can catalyze the desired chemical reaction. These enzymes may be natural or modified through genetic or protein engineering.
Enzymatic reaction: Under appropriate reaction conditions (such as temperature, pH value, substrate concentration, etc.), the starting material and enzyme are mixed together to initiate the enzymatic reaction. Enzymes reduce the activation energy of the reaction by binding to substrates, thereby accelerating the progress of the reaction.
Formation of intermediates: Under the action of enzymes, the starting material undergoes a series of chemical transformations to form intermediates. These intermediates may be one or more, depending on the reaction pathway and enzyme catalytic mechanism.
Further conversion of intermediates: The formed intermediates continue to undergo chemical reactions under the action of enzymes, gradually approaching the structure of the target compound.
Generation of target compound: After a series of enzymatic reactions, deserellin is ultimately produced. At this point, appropriate separation and purification techniques are needed to separate the target compound from the reaction mixture.
Structure identification of the product: Use spectroscopic, chromatographic and other methods to identify the structure of the generated Deserellin, ensuring that its structure meets expectations.
- Chemical equation
For example, if the synthesis of Deslorelin starts from compound A, undergoes catalytic conversion by enzyme E1 to intermediate B, then undergoes catalytic conversion by enzyme E2 to intermediate C, and finally generates Deserellin D, then this process can be roughly expressed as:
A+E1 → B
B+E2 → C
C → D
The arrows here indicate the direction of the enzymatic reaction, while E1 and E2 represent the enzymes involved in the reaction. The actual synthesis pathway may be more complex, involving more steps and enzymes.
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