CETRORELIX Chemical Properties

storage temp. 

-20°C

solubility 

methanol: soluble10%

form 

solid

color 

White to off-white

Water Solubility 

Soluble in water

Safety Information

Risk Statements 

60-63

Safety Statements 

22

WGK Germany 

3

CETRORELIX Usage And Synthesis

Description

Cetrorelix is a synthetic peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with a K_d value of 0.2 nM for radioligand binding to murine LTK- cells expressing human GnRHR. It inhibits the activation of hGnRHR and a downstream luciferase reporter gene in murine LTK- cells by the GnRHR agonist [D-Trp⁶]GnRH (IC₅₀ = 1.2 nM). In vivo, cetrorelix (60 μg per day) reduces tumor volume to 35% of control and decreases serum luteinizing hormone levels by 50% in a human epithelial ovarian cancer mouse xenograft model. Centrorelix (0.5 mg/kg) protects the primordial follicles (PMF) in mouse ovaries from damage induced by cyclophosphamide with 65% to 86% PMF survival compared to 46% PMF survival with a saline control. Formulations containing cetrorelix have been used to prevent ovulation during in vitro fertilization.

Uses

Cetrorelix, a luteinizing hormone releasing hormone receptor (LHRHR) antagonist, was used to study its safety, mechanism of action, metabolism, and efficacy as a therapeutic agent for the treatment of blood cancers such as multiple myeloma (MM). Cetrorelix is used to evaluate its effects on a wide range of physiological processes and malignancies that involve luteinizing hormone releasing hormone receptor signaling pathways involving processes such as steroidogenesis.

Uses

Cetrorelix Acetate is an gonadotropin-releasing hormone antagonist and is used to treat hormone-sensitive cancers of the prostate and breast.

Definition

ChEBI: The acetic acid salt of cetrorelix. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast.

Biochem/physiol Actions

Cetrorelix acetate is a luteinizing hormone releasing hormone receptor antagonist. It causes prepubertal reduction in bone modeling, bone density and bone strength comparable to post-menopausal bone loss.

storage

Store at -20°C

CETRORELIX(145672-81-7)Related Product Information

• CETRORELIX
• CETRORELIX cetrorelix
• Acetylated cetrorelix
• NA
• CETRORELIX ACETATE (Sitraric Acetate)
• Deamidated cetrorelix
• AC-(D-ALA[3-(2-NAPHTHYL)])-[D-PHE(4-CL)]-(D-ALA[3-(3-PYRIDYL)])-SER-TYR-(D-CIT)-LEU-ARG-PRO-D-ALA-NH2, ACETATE
• Cetrorelix trifluoroacetate
• Cetrorelix acetate
• Cetrorelix acetate