| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
GnRH[1]
Targets the gonadotropin-releasing hormone receptor (GnRHR) as a pure antagonist. By blocking the GnRH receptor in the pituitary gland, it prevents the release of both luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This results in a rapid, dose-dependent suppression of gonadal steroidogenesis, particularly the production of testosterone in men. |
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| ln Vitro |
In vitro, Abarelix acetate is characterized by its high affinity binding to the GnRH receptor and its potent antagonism. It blocks GnRH-induced inositol phosphate production and calcium mobilization in GnRH receptor-expressing cells. As a pure antagonist, it does not cause an initial "flare" or surge in gonadotropin release, which is a key advantage over older GnRH agonist drugs.
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| ln Vivo |
In vivo, Abarelix acetate is a highly effective and rapidly acting hormonal therapy. In preclinical and clinical studies, it is used to treat prostate cancer, where it dramatically lowers serum testosterone levels. The onset of its action is rapid (within 8-24 hours of the first dose), and testosterone levels are suppressed to castration levels (often <50 ng/dL) without an initial flare.
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| Enzyme Assay |
Non-cell radioligand binding assays for the GnRH receptor are performed using membranes from pituitary cells or cells expressing the human GnRH receptor. The membranes are incubated with a radiolabeled GnRH agonist (e.g., [¹2⁵I][D-Trp6]-GnRH) and increasing concentrations of Abarelix acetate to determine its Ki, measuring its affinity for the receptor.
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| Cell Assay |
Functional antagonism is assessed in primary pituitary cell cultures or in cell lines expressing the GnRH receptor (e.g., alphaT3-1 or LbetaT2 cells). Cells are pre-incubated with Abarelix before stimulation with a GnRH agonist. The endpoint is typically the inhibition of GnRH-stimulated LH or FSH secretion, measured by ELISA, or the measurement of downstream signaling like inositol phosphate accumulation.
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| Animal Protocol |
In a typical prostate cancer xenograft model in rats or mice, animals are implanted with human prostate cancer cells (e.g., LNCaP). The animals are then given subcutaneous injections of Abarelix acetate (e.g., 100 microg/rat daily). Tumor volume is measured twice weekly, and blood samples are taken to measure serum testosterone levels to confirm the pharmacological effect of the antagonist.
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| ADME/Pharmacokinetics |
Abarelix has a relatively short half-life in humans (about 6-8 hours for the subcutaneous depot formulation). It is administered as a subcutaneous injection. It is classified as a peptide, and like all peptides, it is not orally bioavailable. Its metabolism is not fully characterized but is expected to involve proteolytic degradation.
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| Toxicity/Toxicokinetics |
Abarelix acetate is a prescription drug approved in the US and other countries for the treatment of advanced prostate cancer under the brand name Plenaxis®. Its use is limited due to the risk of severe, immediate-onset allergic reactions (anaphylaxis). Common side effects include hot flashes, injection site pain, sleep disturbances, and gynecomastia.
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| References | |
| Additional Infomation |
Abarelix acetate is an approved drug for prostate cancer, not merely a research tool. It is a "pure" antagonist, meaning it provides immediate hormonal suppression without the initial testosterone surge (flare) associated with GnRH agonists. However, due to allergy concerns, it is typically only used in patients for whom other treatments are not suitable.
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| Molecular Formula |
C74H99CLN14O16
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|---|---|
| Molecular Weight |
1476.11507725716
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| Exact Mass |
1474.705
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| CAS # |
547741-72-0
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| Related CAS # |
Abarelix;183552-38-7
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| PubChem CID |
16141059
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
38
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| Heavy Atom Count |
105
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| Complexity |
2800
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC3=CN=CC=C3)NC(=O)[C@@H](CC4=CC=C(C=C4)Cl)NC(=O)[C@@H](CC5=CC6=CC=CC=C6C=C5)NC(=O)C.CC(=O)O
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| InChi Key |
ZRHCGBCCWJPSQF-JOOIWXSYSA-N
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| InChi Code |
InChI=1S/C72H95ClN14O14.C2H4O2/c1-41(2)32-54(64(93)80-53(17-10-11-30-77-42(3)4)72(101)87-31-13-18-60(87)69(98)78-43(5)63(75)92)81-68(97)58(38-62(74)91)84-70(99)61(37-46-22-27-52(90)28-23-46)86(7)71(100)59(40-88)85-67(96)57(36-48-14-12-29-76-39-48)83-66(95)56(34-45-20-25-51(73)26-21-45)82-65(94)55(79-44(6)89)35-47-19-24-49-15-8-9-16-50(49)33-47;1-2(3)4/h8-9,12,14-16,19-29,33,39,41-43,53-61,77,88,90H,10-11,13,17-18,30-32,34-38,40H2,1-7H3,(H2,74,91)(H2,75,92)(H,78,98)(H,79,89)(H,80,93)(H,81,97)(H,82,94)(H,83,95)(H,84,99)(H,85,96);1H3,(H,3,4)/t43-,53+,54+,55-,56-,57-,58-,59+,60+,61+;/m1./s1
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| Chemical Name |
(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]-methylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide;acetic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO: ≥ 100 mg/mL (67.75 mM)
H2O: 25 mg/mL (16.94 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6775 mL | 3.3873 mL | 6.7745 mL | |
| 5 mM | 0.1355 mL | 0.6775 mL | 1.3549 mL | |
| 10 mM | 0.0677 mL | 0.3387 mL | 0.6775 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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