ChemicalBook--->CAS DataBase List--->145672-81-7

145672-81-7

145672-81-7 Structure

145672-81-7 Structure
IdentificationBack Directory
[Name]

CETRORELIX
[CAS]

145672-81-7
[Synonyms]

Ns 75a
D 20761
Cetrotid
Ovurelix
Sb 075 acetate
Cetrorelix impurity
SB-075 ACETATE;NS-75A
Cetrorelix( x acetate)
Cetrorelix Acetate,SB-075 acetate,NS-75A, >98%
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 acetic acid salt
D-Alaninamide, 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-, acetate (salt)
[Molecular Formula]

C70H92ClN17O14.C2H4O2
[MDL Number]

MFCD08459466
[MOL File]

145672-81-7.mol
[Molecular Weight]

1491.11
Chemical PropertiesBack Directory
[storage temp. ]

-20°C
[solubility ]

methanol: soluble10%
[form ]

solid
[color ]

White to off-white
[Water Solubility ]

Soluble in water
[Sequence]

N-acetyl-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-Ser-Tyr-{Cit}-Leu-Arg-Pro-Ala-NH2
[InChIKey]

KFEFLCOCAHJBEA-YIQVFHPZNA-N
Safety DataBack Directory
[Symbol(GHS) ]

Health Hazard (GHS08)
GHS08
[Signal word ]

Danger
[Hazard statements ]

H360F
[Precautionary statements ]

P201-P280-P308+P313
[Risk Statements ]

60-63
[Safety Statements ]

22
[WGK Germany ]

3
[Storage Class]

6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects
[Hazard Classifications]

Repr. 1B
Hazard InformationBack Directory
[Description]

Cetrorelix is a synthetic peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with a Kd value of 0.2 nM for radioligand binding to murine LTK- cells expressing human GnRHR. It 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. Centrorelix (0.5 mg/kg) protects the primordial follicles (PMF) in mouse ovaries from damage induced by cyclophosphamide (Item No. 13849) with 65% to 86% PMF survival compared to 46% PMF survival with a saline control. Formulations containing cetrorelix have been used to prevent ovulation during in vitro fertilization.
[Uses]

Cetrorelix Acetate is an gonadotropin-releasing hormone antagonist and is used to treat hormone-sensitive cancers of the prostate and breast.
[Definition]

ChEBI: The acetic acid salt of cetrorelix. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast.
[Biochem/physiol Actions]

Cetrorelix acetate is a luteinizing hormone releasing hormone receptor antagonist. It causes prepubertal reduction in bone modeling, bone density and bone strength comparable to post-menopausal bone loss.
[storage]

Store at -20°C
[References]

[1] THOMAS BECKERS  Peter H  Helmut Reil?nder. Characterization of Gonadotropin-Releasing Hormone Analogs Based on a Sensitive Cellular Luciferase Reporter Gene Assay[J]. Analytical biochemistry, 1997, 251 1: Pages 17-23. DOI: 10.1006/abio.1997.2208
[2] T YANO. Inhibition of growth of OV-1063 human epithelial ovarian cancer xenografts in nude mice by treatment with luteinizing hormone-releasing hormone antagonist SB-75.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1994, 91 15: 7090-7094. DOI: 10.1073/pnas.91.15.7090
[3] DROR MEIROW. The GnRH antagonist cetrorelix reduces cyclophosphamide-induced ovarian follicular destruction in mice.[J]. Human reproduction, 2004, 19 6: 1294-1299. DOI: 10.1093/humrep/deh257
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