Cetrorelix Acetate

SKU: orb1301725

Description

Cetrorelix Acetate is a potent GnRH receptor antagonist (IC50 = 1.21 nM). It is widely used in research to inhibit gonadotropin secretion, facilitating studies in endocrinology, oncology, and reproductive biology in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 145672-81-7
• MW: 1491.11
• Purity: 98.00% (May vary between batches)
• Formula: C₇₀H₉₂ClN₁₇O₁₄.xC₂H₄O₂
• SMILES: CC(O)=O.CC(C)C[C@H](NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O
• Target: GNRH Receptor
• Solubility: DMSO:50 mg/mL (33.53 mM)

Bioactivity

• Target IC50:
  GnRH:1.21 nM
• In Vivo:
  Cetrorelix 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.
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• In Vitro:
  GnRH-I antagonist Cetrorelix inhibited growth of ES-2 cell line only at 1000 ng/ml. The incubation of ES-2 ovarian cancer cells in vitro with an GnRH-I antibody inhibited cell proliferation in a time and concentration-dependent manner. GnRH-I may function as an autocrine growth factor in this ovarian cancer cell line .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GnRHR, GNRH Receptor, GNRHReceptor, SB 75, SB75, SB-75

Compound Identifiers

PubChem CID

25078429