| Identification | Back 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 Properties | Back 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 Data | Back Directory | [Symbol(GHS) ]
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 Information | Back 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.1 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.2 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.3 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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