MedChemExpress - Model Teverelix -151272-78-5

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].

Teverelix

MCE China：Teverelix

Brand：MedChemExpress (MCE)

Cat. No.HY-105173

CAS：151272-78-5

Synonyms：EP 24332

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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].

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].

References：

[1]. MacLean CM, et al. Pharmacokinetic, Safety, and Pharmacodynamic Properties of Teverelix Trifluoroacetate, a Novel Gonadotropin-Releasing Hormone Antagonist, in Healthy Adult Subjects. Clin Pharmacol Drug Dev. 2022 Feb;11(2):257-269. [Content Brief]

[2]. Sperduti S, et al. GnRH Antagonists Produce Differential Modulation of the Signaling Pathways Mediated by GnRH Receptors. Int J Mol Sci. 2019 Nov 7;20(22):5548. [Content Brief]

[3]. Deghenghi R, et al. Antarelix (EP 24332) a novel water soluble LHRH antagonist. Biomed Pharmacother. 1993;47(2-3):107-10. [Content Brief]

[4]. Fraser HM, et al. Initiation of high dose gonadotrophin-releasing hormone antagonist treatment during the late follicular phase in the macaque abolishes luteal function irrespective of effects upon the luteinizing hormone surge. Hum Reprod. 1997 Mar;12(3):430-5. [Content Brief]

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MedChemExpress - Model Teverelix -151272-78-5

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Teverelix