Abarelix

Modify Date: 2024-01-04 16:08:05

Abarelix Structure
Abarelix structure
 Common Name Abarelix
CAS Number 183552-38-7 Molecular Weight 1416.063
Density 1.3±0.1 g/cm3 Boiling Point 1688.4±65.0 °C at 760 mmHg
Molecular Formula C72H95ClN14O14 Melting Point N/A
MSDS N/A Flash Point 974.9±34.3 °C

 Use of Abarelix


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

 Names

Name abarelix
Synonym More Synonyms

 Abarelix Biological Activity

Description Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
Related Catalog
In Vitro Abarelix (30 and 300 µg/mL) and cetrorelix cause significantly increased histamine release[1]. Abarelix is the firstGnRH 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].
References

[1]. Koechling W, et al. Degarelix, a novel GnRH antagonist, causes minimal histamine release compared with cetrorelix, abarelix and ganirelix 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 gonadotropin-releasing hormone antagonist for prostate cancer. Future Oncol. 2006 Dec;2(6):677-96.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 1688.4±65.0 °C at 760 mmHg
Molecular Formula C72H95ClN14O14
Molecular Weight 1416.063
Flash Point 974.9±34.3 °C
Exact Mass 1414.684082
PSA 424.98000
LogP 5.18
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.601
Storage condition -20°C

 Synonyms

Carbamic acid,acetyldithio-,methyl ester
Abarelix
Carbamodithioic acid,acetyl-,methyl ester
Ac-D-Nal-[D-(pCl)Phe]-D-Pal-Ser-[Nα-Me-Tyr]-D-Asn-Leu-ILys-Pro-DAla-NH2
acetyl-dithiocarbamic acid methyl ester
Abarelix Acetate
N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide
(2R)-N-[(2S)-1-{[(2S)-1-[(2S)-2-{[(2R)-1-Amino-1-oxopropan-2-yl]carbamoyl}pyrrolidin-1-yl]-6-(isopropylamino)-1-oxohexan-2-yl]amino}-4-methyl-1-oxopentan-2-yl]-2-{[(2S,5S,8R,11R,14R)-11-(4-chlorobenzyl)-2-(4-hydroxybenzyl)-5-(hydroxymethyl)-3-methyl-14-(2-naphthylmethyl)-4,7,10,13,16-pentaoxo-8-(pyridin-3-ylmethyl)-3,6,9,12,15-pentaazaheptadecan-1-oyl]amino}succinamide (non-preferred name)
Acetyl-dithiocarbamidsaeure-methylester
(2R)-N-[(2S)-1-{[(2S)-1-[(2S)-2-{[(2R)-1-Amino-1-oxo-2-propanyl]carbamoyl}-1-pyrrolidinyl]-6-(isopropylamino)-1-oxo-2-hexanyl]amino}-4-methyl-1-oxo-2-pentanyl]-2-{[(2S,5S,8R,11R,14R)-11-(4-chlorobe nzyl)-2-(4-hydroxybenzyl)-5-(hydroxymethyl)-3-methyl-14-(2-naphthylmethyl)-4,7,10,13,16-pentaoxo-8-(3-pyridinylmethyl)-3,6,9,12,15-pentaazaheptadecan-1-oyl]amino}succinamide
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