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Abarelix

Catalog No. T10217L CAS 183552-38-7

Synonyms: PPI 149, 阿巴瑞克, R3827

Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, which is used for prostate cancer treatment.

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Abarelix, CAS 183552-38-7

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Purity: 98%

Biological Description

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Description

Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, which is used for prostate cancer treatment.

In vitro

Abarelix (30 and 300 µg/mL) causes significantly increased histamine release[1]. Abarelix demonstrates to promptly and substantially reduce follicle-stimulating hormone levels to lower than LHRH agonist. Abarelix is the first GnRH antagonist to be developed which 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 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].

Synonyms	PPI 149, 阿巴瑞克, R3827
Molecular Weight	1416.06
Formula	C72H95ClN14O14
CAS No.	183552-38-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 14.2 mg/mL (10.03 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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. 2. Kirby RS, et al. Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. 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.

Related compound libraries

This product is contained In the following compound libraries：

Peptide Compound Library Inhibitor Library Drug Repurposing Compound Library FDA-Approved Drug Library Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library

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Keywords

Abarelix 183552-38-7 G蛋白偶联受体 GNRH Receptor GNRHR R 3827 R3827 GnRH Receptor PPI-149 Gonadotropin releasing hormone receptor PPI 149 PPI149 inhibit R-3827 Inhibitor inhibitor

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