151272-78-5

151272-78-5 structure

Name: antarelix
Chemical Name: teverelix
CAS Number: 151272-78-5
Molecular Formula: C₇₄H₁₀₀ClN₁₅O₁₄
Molecular Weight: 1459.131
Catalog: Signaling Pathways GPCR/G Protein GNRH Receptor
Create Date: 2021-09-12 11:21:01
Modify Date: 2024-01-13 12:20:07
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].

Name	teverelix
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

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	Signaling Pathways >> GPCR/G Protein >> GNRH Receptor Research Areas >> Cancer Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
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.