Description

Product Description

Cetrorelix diacetate (CAS 130143-01-0) is a synthetic peptide and a potent gonadotropin-releasing hormone (GnRH) receptor antagonist. By selectively binding to GnRH receptors, Cetrorelix diacetate blocks the downstream release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), making it an essential tool for reproductive and endocrine research.

Background and Research Significance

GnRH plays a central role in regulating the hypothalamic-pituitary-gonadal (HPG) axis. By antagonizing the GnRH receptor, Cetrorelix diacetate allows researchers to:

• Investigate hormone regulation mechanisms in preclinical models.

• Study fertility control and reproductive endocrinology.

• Develop therapeutic strategies for hormone-dependent diseases.

The high potency of Cetrorelix diacetate (IC50 1.21 nM) ensures effective inhibition of gonadotropin release in in vitro and in vivo models, enabling reproducible studies of hormone signaling, fertility modulation, and endocrine pharmacology.

Chemical Properties and Structure

• Compound Class: Synthetic peptide GnRH receptor antagonist

• Target: GnRH receptor

• Mechanism: Competitive inhibition of receptor binding

• Activity: Potent receptor antagonism (IC50 1.21 nM)

• Stability: Lyophilized peptide with extended shelf life

• Applications: Reproductive biology, endocrine research, fertility modulation

Cetrorelix diacetate’s synthetic design provides high purity, structural integrity, and reproducible pharmacological activity, essential for preclinical studies.

Product Specifications

The specifications ensure high purity, consistent potency, and reliable receptor antagonism, enabling robust preclinical studies.

Mechanism of Action & Research Applications

Mechanism of Action

Cetrorelix diacetate functions by competitively binding to the GnRH receptor, preventing natural GnRH from activating the receptor. This inhibition results in:

1. Suppression of LH and FSH Release: Reduces gonadotropin secretion from the pituitary.

2. Downregulation of Steroid Hormone Synthesis: Alters ovarian/testicular steroidogenesis in preclinical models.

3. Reversible Hormone Modulation: Allows controlled studies of reproductive cycles and fertility parameters.

Its IC50 of 1.21 nM demonstrates high potency, allowing researchers to modulate the HPG axis precisely.

Research Applications

1. Reproductive Biology Research
Investigate gonadotropin regulation, ovulation, and fertility in rodent and in vitro models.

2. Endocrine Studies
Study hormone signaling pathways, feedback loops, and receptor pharmacology.

3. Fertility Modulation
Used in experiments assessing assisted reproductive technologies (ART), oocyte maturation, and luteal phase control.

4. Hormone-Dependent Disease Research
Facilitates studies on prostate cancer, breast cancer, and other hormone-sensitive tumors.

5. Mechanistic Endocrinology
Enables exploration of GnRH receptor signaling, receptor desensitization, and downstream gene expression.

6. Translational Research
Data supports development of GnRH antagonist-based therapies for fertility control and hormone-dependent disorders.

7. In Vitro Pharmacology
Cetrorelix diacetate is used in cultured pituitary cells and reproductive tissue assays to evaluate receptor antagonism.

8. Comparative Peptide Studies
Allows comparison with other GnRH agonists and antagonists to optimize experimental outcomes.

9. Dose-Response Analysis
High potency permits precise titration in preclinical models to study physiological effects.

10. Laboratory Protocol Development
Supports the design of robust experimental protocols in reproductive and endocrine research.

Side Effects (For Reference in Research Models)

Preclinical observations include:

• Hormonal Suppression: Dose-dependent reduction in LH and FSH levels.

• Reproductive Cycle Modulation: Temporary disruption of estrous or spermatogenic cycles in animal models.

• Species-Specific Variability: Responses may differ between rodents and non-human primates.

• Injection Site Effects: Mild local irritation may occur in subcutaneous administration.

• Pharmacokinetic Considerations: Stable in lyophilized form; avoid repeated freeze-thaw cycles.

These observations are strictly for laboratory research reference. Cetrorelix diacetate is not for human or veterinary use.

Disclaimer

For laboratory research use only. Not for human or veterinary use.

Keywords

• Cetrorelix diacetate CAS 130143-01-0

• GnRH receptor antagonist peptide

• SB-075 diacetate research peptide

• GMP-grade Cetrorelix

• Reproductive biology research peptide

• Fertility modulation peptide

• Laboratory endocrine research peptide

• Preclinical hormone regulation peptide

• Synthetic GnRH antagonist peptide

• Research use only reproductive agent