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130143-01-0

130143-01-0 Structure

130143-01-0 Structure
IdentificationMore
[Name]

Cetrorelix acetate
[CAS]

130143-01-0
[Synonyms]

N-Acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N5-(aminocarbonyl)-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaninamide diacetate
[Molecular Formula]

C70H92N17O14
[MDL Number]

MFCD00884467
[Molecular Weight]

1551.16
[MOL File]

130143-01-0.mol
Chemical PropertiesBack Directory
[storage temp. ]

under inert gas (nitrogen or Argon) at 2-8°C
[solubility ]

DMSO:50.0(Max Conc. mg/mL);33.53(Max Conc. mM)
Water:2.0(Max Conc. mg/mL);1.34(Max Conc. mM)
[Sequence]

Ac-3-(2-naphthyl)-D-Ala-4-Chloro-D-Phe-3(3-pyridyl)-D-Ala-Ser-Tyr-D-Cit-Leu-
[InChIKey]

JUIDLEJONVXAMD-SFKTYWRYNA-N
[CAS DataBase Reference]

130143-01-0(CAS DataBase Reference)
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P280-P301+P312-P302+P352-P305+P351+P338
Hazard InformationBack Directory
[Uses]

Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM[1].
[Clinical Use]

Cetrorelix acetate is an analogue of GnRH with amino acid substitutions at residues 1, 2, 3, 6, and 10 and differing from ganirelix at amino acids 1, 6, and 8. Each of these substitutions are synthetic, non-DNA-directed amino acids and, like ganirelix acetate, impart GnRH antagonist activity to cetrorelix acetate. This drug also is marketed for use in women undergoing assisted reproductive therapy (ART) procedures, in which it is necessary to control their LH surge. This allows the follicles to develop to a size, as determined by ultrasound, that increases the success of timed insemination and oocyte retrieval for IVF. Like ganirelix acetate, cetrorelix acetate has an advantage over GnRH agonists, such as leuprolide acetate, because it reduces the fertility therapy cycle to days rather than weeks.
[References]

[1] Beckers T et al. Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay. Anal Biochem. 1997 Aug 15;251(1):17-23. DOI:10.1006/abio.1997.2208
[2] Gründker C et al. Role of gonadotropin-releasing hormone (GnRH) in ovarian cancer. Reprod Biol Endocrinol. 2003 Oct 7;1:65. DOI:10.1186/1477-7827-1-65
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