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Purity: =99%
| Targets |
The primary molecular target of Buserelin Acetate is the gonadotropin-releasing hormone (GnRH) receptor, also known as the LHRH receptor. As a potent agonist of the GnRH receptor, buserelin binds to and activates the receptor on pituitary gonadotroph cells. Initial stimulation leads to a transient increase in the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn stimulates the production of sex hormones. However, with continued administration, buserelin causes downregulation of GnRH receptors and desensitization of the pituitary, leading to a sustained reduction in LH and FSH secretion and consequently a decrease in sex hormone levels. This chemical castration effect is the basis for its use in hormone-sensitive cancers.
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| ln Vitro |
In vitro studies of Buserelin Acetate have demonstrated its potent agonist activity at the GnRH receptor. The compound binds to GnRH receptors on pituitary cells and stimulates the release of LH and FSH. In vitro assays typically involve treatment of cultured pituitary cells with buserelin followed by measurement of LH and FSH secretion. The compound has been shown to be a potent agonist of LH-releasing hormone. Receptor binding studies have characterized the affinity of buserelin for the GnRH receptor.
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| ln Vivo |
In vivo studies of Buserelin Acetate have demonstrated its efficacy in reducing sex hormone levels and treating hormone-sensitive cancers and other conditions. The compound is administered via subcutaneous injection or as a nasal spray. Buserelin has been shown to effectively reduce testosterone levels in prostate cancer patients and estrogen levels in breast cancer and endometriosis patients, leading to disease regression and improved clinical outcomes. The compound has been used in the treatment of prostate cancer, breast cancer, endometriosis, and uterine fibroids.
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| Enzyme Assay |
In vitro receptor binding assays for Buserelin Acetate typically involve studying its interaction with the GnRH receptor. Radioligand binding assays using labeled GnRH or labeled buserelin can be performed to measure the binding affinity (IC50 or Ki) of the compound for the GnRH receptor. Functional assays, such as LH and FSH secretion assays using pituitary cell cultures, can be used to evaluate the agonist activity of the compound. These assays typically involve treatment of cells with buserelin followed by measurement of hormone release using immunoassays.
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| Cell Assay |
In vitro cell-based assays for Buserelin Acetate typically involve treatment of cultured pituitary cells with the compound followed by assessment of GnRH receptor activation. Cells are treated with buserelin, and the release of LH and FSH is measured using ELISA or other immunoassay techniques. Dose-response experiments are performed to determine the potency (EC50) of the compound in stimulating hormone release. Additionally, receptor binding assays using cells expressing GnRH receptors can be performed to evaluate the affinity of buserelin for the receptor.
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| Animal Protocol |
In vivo animal studies for Buserelin Acetate typically involve administration to animal models to evaluate its effects on hormone levels and disease progression. In prostate cancer models, buserelin is administered to tumor-bearing animals to assess tumor growth inhibition and reduction in testosterone levels. In endometriosis models, the compound is used to evaluate its effects on endometrial tissue growth and hormone levels. Typical endpoints include measurement of serum hormone levels, tumor volume measurement, and survival analysis.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Buserelin Acetate include its absorption, distribution, metabolism, and excretion characteristics. The compound has a molecular formula of C62H90N16O15 and a molecular weight of 1299.48. It has a melting point of 186-188°C. Buserelin can be administered via various routes, including subcutaneous injection and nasal spray. The compound is metabolized through proteolytic degradation and excreted primarily via the kidneys.
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| Toxicity/Toxicokinetics |
The toxicity profile of Buserelin Acetate has been extensively evaluated in preclinical and clinical studies. Common adverse effects include those related to the initial hormone surge and the subsequent reduction in sex hormone levels, which may cause hot flashes, decreased libido, and other symptoms of hormonal deprivation. Long-term use may be associated with bone density loss and other metabolic effects. The compound is contraindicated in patients with certain medical conditions.
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| Additional Infomation |
Buserelin acetate is an organic molecular entity. It is a potent synthetic analog of gonadotropin-releasing hormone, with residue 6 replaced by D-serine, residue 10 replaced by glycine, and other modifications. See also: Buserelin (with active moiety).
Buserelin Acetate (CAS 68630-75-1) is a synthetic analogue of GnRH and a potent agonist of LH-releasing hormone. It is used as an antineoplastic (hormonal) agent for the treatment of prostate cancer, breast cancer, endometriosis, uterine fibroids, and other hormone-responsive diseases. The compound can be administered via subcutaneous injection or as a nasal spray. It has a molecular formula of C62H90N16O15 and a molecular weight of 1299.48. Buserelin functions via binding to GnRH receptors, causing downregulation and suppression of sex hormone production. |
| Molecular Formula |
C60H86N16O13.C2H4O2
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|---|---|
| Molecular Weight |
1299.4762
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| Exact Mass |
1238.656
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| CAS # |
68630-75-1
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| Related CAS # |
68630-75-1;68630-75-1 (acetate);
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| PubChem CID |
50224
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Melting Point |
186-188°C
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| Index of Refraction |
1.671
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| LogP |
0.7
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
93
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| Complexity |
2480
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CCNC([C@@H]1CCCN1C([C@@H](NC([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H]2CCC(N2)=O)=O)CC3=CN=CN3)=O)CC4=CNC5=CC=CC=C45)=O)CO)=O)CC6=CC=C(O)C=C6)=O)COC(C)(C)C)=O)CC(C)C)=O)CCCNC(N)=N)=O)=O.CC(O)=O
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| InChi Key |
PYMDEDHDQYLBRT-DRIHCAFSSA-N
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| InChi Code |
InChI=1S/C60H86N16O13.C2H4O2/c1-7-64-57(87)48-15-11-23-76(48)58(88)41(14-10-22-65-59(61)62)69-51(81)42(24-33(2)3)70-56(86)47(31-89-60(4,5)6)75-52(82)43(25-34-16-18-37(78)19-17-34)71-55(85)46(30-77)74-53(83)44(26-35-28-66-39-13-9-8-12-38(35)39)72-54(84)45(27-36-29-63-32-67-36)73-50(80)40-20-21-49(79)68-40;1-2(3)4/h8-9,12-13,16-19,28-29,32-33,40-48,66,77-78H,7,10-11,14-15,20-27,30-31H2,1-6H3,(H,63,67)(H,64,87)(H,68,79)(H,69,81)(H,70,86)(H,71,85)(H,72,84)(H,73,80)(H,74,83)(H,75,82)(H4,61,62,65);1H3,(H,3,4)/t40-,41-,42-,43-,44-,45-,46-,47+,48-;/m0./s1
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| Chemical Name |
acetic acid;(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-[(2-methylpropan-2-yl)oxy]-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 | 0.7695 mL | 3.8477 mL | 7.6954 mL | |
| 5 mM | 0.1539 mL | 0.7695 mL | 1.5391 mL | |
| 10 mM | 0.0770 mL | 0.3848 mL | 0.7695 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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