antarelix

Modify Date: 2024-01-13 12:20:07

antarelix Structure
antarelix structure
Common Name antarelix
CAS Number 151272-78-5 Molecular Weight 1459.131
Density 1.3±0.1 g/cm3 Boiling Point 1692.9±65.0 °C at 760 mmHg
Molecular Formula C74H100ClN15O14 Melting Point N/A
MSDS N/A Flash Point 977.6±34.3 °C

 Use of antarelix


Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer[1][2].

 Names

Name teverelix
Synonym More Synonyms

 antarelix Biological Activity

Description Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer[1][2].
Related Catalog
In Vitro Teverelix (10 nM, 45 mins) inhibits GnRH-induced intracellular Ca2+ increase in HEK293/GnRHR cells[2]. Teverelix (0.1 nM-1 μM, 45 mins) inhibits GnRH-induced cAMP accumulation in HEK293/GnRHR cells[2]. Teverelix (10 nM-1 μM, 15 mins) inhibits GnRH-induced pERK1/2 and pCREB activation in HEK293/GnRHR cells[2]. Teverelix inhibits histamine release in a peritoneal rat mast cell, with an EC50value of 81 μg/mL[3]. Western Blot Analysis[2] Cell Line: HEK293/GnRHR cells Concentration: 10 nM, 100 nM, 1 μM Incubation Time: 15 mins Result: Inhibited GnRH-induced pERK1/2 and pCREB activation.
In Vivo Teverelix (3-300 μg/kg, intramuscular injection) inhibits testosterone in rats[3]. Teverelix (1 mg/kg, s.c, daily for 3 days) abolishes luteal function in stumptailed macaques[4]. Animal Model: Rats[3] Dosage: 300, 100, 30, 10 and 3 μg/kg Administration: Intramuscular injection Result: Showed dose-response and time-course of testosterone inhibitory activity.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 1692.9±65.0 °C at 760 mmHg
Molecular Formula C74H100ClN15O14
Molecular Weight 1459.131
Flash Point 977.6±34.3 °C
Exact Mass 1457.726318
LogP 4.49
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.597

 Synonyms

7079
D19V7048JK
N-Acetyl-3-(2-naphthyl)-D-alanyl-p-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L-tyrosyl-N6-carbamoyl-D-lysyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide
(2S)-N-[(2R)-1-Amino-1-oxo-2-propanyl]-1-[(2S,5S,8R,11S,14S,17R,20R,23R)-8-[4-(carbamoylamino)butyl]-20-(4-chlorobenzyl)-11-(4-hydroxybenzyl)-14-(hydroxymethyl)-5-isobutyl-2-[4-(isopropylamino)butyl]-23-(2-naphthylmethyl)-4,7,10,13,16,19,22,25-octaoxo-17-(3-pyridinylmethyl)-3,6,9,12,15,18,21,24-octaazahexacosan-1-oyl]-2-pyrrolidinecarboxamide
teverelix
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