| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: =99.53%
| Targets |
Deslorelin targets the gonadotropin-releasing hormone receptor (GnRHR) on the surface of cells in the pituitary gland. As a potent agonist, it binds to and activates the GnRH receptor, leading to the initial release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). However, with continued administration, deslorelin causes downregulation of GnRH receptors and desensitization of the pituitary gland. This results in decreased secretion of gonadotropins and subsequent suppression of sex hormone production, including testosterone and estrogen.
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| ln Vitro |
In vitro, deslorelin binds to GnRH receptors on pituitary cells with high affinity, stimulating the release of FSH and LH. Its activity is assessed using cell-based assays, where pituitary cells or GnRH receptor-expressing cell lines are treated with varying concentrations of deslorelin, and the release of gonadotropins is measured by ELISA or radioimmunoassay. The compound's potency is characterized by its EC50 for gonadotropin release. Deslorelin is significantly more potent than natural GnRH due to its structural modifications.
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| ln Vivo |
In vivo, deslorelin is used to induce ovulation and as a contraceptive in humans. In male animals, it decreases expression of GnRH receptors and levels of testosterone, decreasing the volume of the testes and prostate. In male animals, deslorelin is used to instill sterility. In female animals, it suppresses estrogen production, preventing ovulation. The compound's ability to suppress sex hormone production makes it useful for the treatment of hormone-dependent conditions, including prostate cancer, endometriosis, and uterine fibroids.
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| Enzyme Assay |
The in vitro activity of deslorelin is assessed using radioligand binding assays and functional assays. For receptor binding, membrane preparations from cells expressing the GnRH receptor are incubated with a radiolabeled GnRH analog in the presence of varying concentrations of deslorelin. The displacement of the radiolabeled ligand is measured to determine the Ki. For functional assays, pituitary cells or GnRH receptor-expressing cell lines are treated with deslorelin, and the release of FSH and LH is measured by ELISA or radioimmunoassay. The EC50 is determined from dose-response curves.
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| Cell Assay |
For cellular assays, primary pituitary cell cultures or GnRH receptor-expressing cell lines (e.g., LβT2 cells) are cultured in appropriate media. Cells are treated with various concentrations of deslorelin (typically 0.1 pM to 100 nM) for defined periods (1-24 hours). Gonadotropin release (LH and FSH) in the culture medium is measured by ELISA or radioimmunoassay. The expression of GnRH receptor mRNA and protein is analyzed by qPCR or Western blotting to assess receptor downregulation. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo, deslorelin is typically administered via subcutaneous or intramuscular injection in humans and animals. In animal models, the compound is used to induce ovulation, suppress fertility, or treat hormone-dependent conditions. Dosing regimens vary depending on the species and indication. Efficacy is assessed by measuring hormone levels (testosterone, estrogen, LH, FSH) in blood samples. In toxicological studies, the compound is administered at various doses, and effects on reproductive organs, hormone levels, and general toxicity are assessed.
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| ADME/Pharmacokinetics |
Deslorelin is a synthetic peptide with a molecular weight of approximately 1282.42 g/mol. It is typically supplied as the acetate salt for enhanced stability and solubility. The compound should be stored as a lyophilized powder at -20°C under desiccated conditions. For administration, it is reconstituted in sterile water or saline. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Specific toxicity data for deslorelin is not detailed in the provided search results. As a GnRH agonist, it can cause side effects related to sex hormone suppression, including hot flashes, decreased libido, and bone density loss with long-term use. The compound is intended for research and therapeutic use under appropriate regulatory oversight. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile for different applications.
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| Additional Infomation |
Delorelin is an oligopeptide. Delorelin acetate is an injectable gonadotropin-releasing hormone superagonist, also known as an LHRH agonist. It inhibits the production of sex hormones. Delorelin is a synthetic nonapeptide analog of natural gonadotropin-releasing hormone (GnRH) and has potential antitumor activity. Delorelin binds to and activates pituitary GnRH receptors. Long-term continuous use of goserelin in men leads to desensitization of pituitary GnRH receptors and inhibits the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), resulting in a significant decrease in testosterone levels; long-term use in women leads to a decrease in estradiol levels. (NCI04) See also: Delorelin acetate (in salt form); Delorelin; Delorelin acetate (ingredient).
Deslorelin is a GnRH agonist that has been used in veterinary medicine for the management of reproductive disorders and as a contraceptive. In human medicine, it has been studied for the treatment of hormone-dependent conditions, including prostate cancer and endometriosis. Deslorelin is also used in research to study the regulation of the hypothalamic-pituitary-gonadal axis. It is not approved for human use in many countries but is available for research purposes. |
| Molecular Formula |
C64H83N17O12
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|---|---|
| Molecular Weight |
1282.4505
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| Exact Mass |
1281.64
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| CAS # |
57773-65-6
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| Related CAS # |
Deslorelin Acetate;82318-06-7
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| PubChem CID |
25077495
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
1783.4ºC at 760 mmHg
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| Flash Point |
1032.4ºC
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| Index of Refraction |
1.710
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| LogP |
0.77
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
32
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| Heavy Atom Count |
93
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| Complexity |
2610
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| Defined Atom Stereocenter Count |
9
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| SMILES |
O=C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)N([H])C([C@]([H])(C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])O[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)N([H])C([C@]([H])(C([H])([H])C1=C([H])N=C([H])N1[H])N([H])C([C@]1([H])C([H])([H])C([H])([H])C(N1[H])=O)=O)=O)=O)=O)=O)=O)=O)N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])C([H])([H])C([H])([H])[H])=O
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| InChi Key |
GJKXGJCSJWBJEZ-XRSSZCMZSA-N
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| InChi Code |
InChI=1S/C64H83N17O12/c1-4-68-62(92)53-16-10-24-81(53)63(93)46(15-9-23-69-64(65)66)74-56(86)47(25-35(2)3)75-58(88)49(27-37-30-70-43-13-7-5-11-41(37)43)77-57(87)48(26-36-17-19-40(83)20-18-36)76-61(91)52(33-82)80-59(89)50(28-38-31-71-44-14-8-6-12-42(38)44)78-60(90)51(29-39-32-67-34-72-39)79-55(85)45-21-22-54(84)73-45/h5-8,11-14,17-20,30-32,34-35,45-53,70-71,82-83H,4,9-10,15-16,21-29,33H2,1-3H3,(H,67,72)(H,68,92)(H,73,84)(H,74,86)(H,75,88)(H,76,91)(H,77,87)(H,78,90)(H,79,85)(H,80,89)(H4,65,66,69)/t45-,46-,47-,48-,49+,50-,51-,52-,53-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7798 mL | 3.8988 mL | 7.7976 mL | |
| 5 mM | 0.1560 mL | 0.7798 mL | 1.5595 mL | |
| 10 mM | 0.0780 mL | 0.3899 mL | 0.7798 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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