
Biological Activity
Potent gonadotropin-releasing hormone (GnRH) receptor antagonist (KD = 0.202 nM, IC50 = 1.21 nM). Suppresses production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland, which inhibits ovulation. Exhibits antiproliferative effects and displays efficacy against hormone-sensitive cancers in vivo. Also exhibits anxiolytic and antidepressant activity in vivo.
Technical Data
M. Wt | 1491.11 |
Formula | C70H92ClN17O14.C2H4O2 |
Sequence |
XFASYXLRPA (Modifications: X-1 = D-2-Nal and N-terminal Ac, Phe-2 = D-(4-Cl-Phe), Ala-3 = D-(3-Pyridyl-Ala), X-6 = D-Cit, Ala-10 = D-Ala and C-terminal amide) |
Storage | Store at -20°C |
CAS Number | 145672-81-7 |
PubChem ID | 25078429 |
InChI Key | KFEFLCOCAHJBEA-ANRVCLKPSA-N |
Smiles | CC(O)=O.CC(C)C[C@H](NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@@H](CC1=CN=CC=C1)NC(=O)[C@@H](CC1=CC=C(Cl)C=C1)NC(=O)[C@@H](CC1=CC2=C(C=CC=C2)C=C1)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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solubility | Soluble in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1491.11. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 0.67 mL | 3.35 mL | 6.71 mL |
5 mM | 0.13 mL | 0.67 mL | 1.34 mL |
10 mM | 0.07 mL | 0.34 mL | 0.67 mL |
50 mM | 0.01 mL | 0.07 mL | 0.13 mL |
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References
References are publications that support the products' biological activity.
Beckers et al (1997) Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay. Anal.Biochem. 251 17 PMID: 9300077
Grundker and Emons (2003) Role of gonadotropin-releasing hormone (GnRH) in ovarian cancer. Reprod.Biol.Endocrinol. 1 65 PMID: 14594454
Telegdy et al (2009) Effects of the LHRH antagonist cetrorelix on the brain function in mice. Neuropeptides 43 229 PMID: 19375162
Keywords: Cetrorelix Acetate, supplier, Potent, GnRH, antagonists, Peptide, Receptors, Gonadotropin-releasing, Hormone, gonadotrophin, Gonadotrophin-Releasing, Hormone, Receptors, Gonadotrophin-Releasing, Hormone, Receptors, Tocris Bioscience