Abarelix
Based on 1 publication(s) in Google Scholar
Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 183552-38-7
- Formula: C72H95ClN14O14
- Molecular Weight:1416.06
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Abarelix
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Customer Validation & Images
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WB
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
3.5 nM
Compound: 4 (Abarelix)
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Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
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[PMID: 11462984] |
Abarelix (30 and 300 µg/mL) causes significantly increased histamine release[1]. Abarelix is the first GnRH antagonist to be developed, and can produce rapid and sustained decreases in testosterone to castrate levels without the need for co-administration of an antiandrogen, and with a very low complication rate in the short term[2]. Abarelix demonstrates to promptly and substantially reduce follicle-stimulating hormone levels to lower than LHRH agonist. Abarelix does not cause a surge in serum testosterone that can precipitate a flare phenomenon or worsening of disease, particularly dangerous for patients with metastatic, symptomatic disease, and produces medical castration more quickly[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 183552-38-7
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Appearance Solid
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Molecular Weight 1416.06
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Formula C72H95ClN14O14
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Color White to off-white
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Synonyms
R3827; PPI 149
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Sequence Shortening
Ac-{d-2-Nal}-{d-4-Cpa}-{d-3-Pal}-S-{NMyr}-{d-Asp}-L-K(ipr)-P-{d-Ala}-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Am J Physiol Endocrinol Metab
Erythropoietin-producing hepatocellular receptor A7 restrains estrogen negative feedback of luteinizing hormone via ephrin A5 in the hypothalamus of female rats. [Abstract]2020 Jul 1;319(1):E81-E90. PMID: 32396496
Abarelix purchased from MedChemExpress. Usage Cited in: Am J Physiol Endocrinol Metab. 2020 Jul 1;319(1):E81-E90. [Abstract]
EPHA7, ERα, and ERβ protein expression in the hypothalamus of abarelix-treated rats injected with EPHA7-Fc.
Solvent & Solubility
DMSO : 100 mg/mL (70.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 42 mg/mL (29.66 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Koechling W, et al. A novel GnRH antagonist, causes minimal histamine release compared with abarelix in an ex vivo model of human skin samples. Br J Clin Pharmacol. 2010 Oct;70(4):580-7. [Content Brief]
[2]. Kirby RS, et al. Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. [Content Brief]
[3]. Debruyne F, et al. Abarelix for injectable suspension: first-in-class releasing hormone antagonist for prostate cancer. Future Oncol. 2006 Dec;2(6):677-96. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.7062 mL | 3.5309 mL | 7.0618 mL | 17.6546 mL |
| 5 mM | 0.1412 mL | 0.7062 mL | 1.4124 mL | 3.5309 mL | |
| 10 mM | 0.0706 mL | 0.3531 mL | 0.7062 mL | 1.7655 mL | |
| 15 mM | 0.0471 mL | 0.2354 mL | 0.4708 mL | 1.1770 mL | |
| 20 mM | 0.0353 mL | 0.1765 mL | 0.3531 mL | 0.8827 mL | |
| 25 mM | 0.0282 mL | 0.1412 mL | 0.2825 mL | 0.7062 mL | |
| DMSO | 30 mM | 0.0235 mL | 0.1177 mL | 0.2354 mL | 0.5885 mL |
| 40 mM | 0.0177 mL | 0.0883 mL | 0.1765 mL | 0.4414 mL | |
| 50 mM | 0.0141 mL | 0.0706 mL | 0.1412 mL | 0.3531 mL | |
| 60 mM | 0.0118 mL | 0.0588 mL | 0.1177 mL | 0.2942 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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