Cetrorelix Acetate

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Cat.No. 3536 - Cetrorelix Acetate | Ac-D-2-Nal-D-(4-Cl-Phe)-D-(3-Pyridyl-Ala)-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2.CH3CO2H | CAS No. 145672-81-7
Description: Potent GnRH receptor antagonist
Datasheet
Citations
Literature

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

SolubilitySoluble 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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Safety Datasheet

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


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Keywords: Potent GnRH antagonists Peptide Receptors Gonadotropin-releasing Hormone gonadotrophin Gonadotrophin-Releasing Hormone Receptors

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GPCR

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Peptide Hormone Receptors

Peptide Hormone Receptors Product Listing

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