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Ozarelix

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

Ozarelix is a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. Mechanistically, LHRH antagonists exert rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones and would therefore be expected to be effective in a variety of hormonally dependent disease states including ovarian cancer, prostate cancer, BPH, infertility, uterine myoma and endometriosis. BPH is a non-cancerous enlargement of the prostate that is caused by testosterone. Unlike LHRH agonists, ozarelix has the potential to reduce testosterone just enough to reduce both prostate size and symptoms without the severe side effects associated with a reduction in testosterone.

Category

Peptide Inhibitors

Catalog number

BAT-016127

CAS number

295350-45-7

Molecular Formula

C72H96ClN17O14

Molecular Weight

1459.11

Specification
Reference Reading

IUPAC Name

(2S)-1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]-methylamino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-(carbamoylamino)hexanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-N-[(2R)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide

Synonyms

D 63153; D-63 153; D-63153; D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-N6-(aminocarbonyl)-D-lysyl-L-norleucyl-L-arginyl-L-prolyl-

Density

1.4±0.1 g/cm3

Sequence

XXXSYXXRPA

InChI

InChI=1S/C72H96ClN17O14/c1-5-6-17-52(63(96)85-54(19-12-33-79-71(75)76)70(103)90-34-13-20-59(90)67(100)81-42(2)61(74)94)83-62(95)53(18-9-10-32-80-72(77)104)84-68(101)60(39-45-24-29-51(93)30-25-45)89(4)69(102)58(41-91)88-66(99)57(38-47-14-11-31-78-40-47)87-65(98)56(36-44-22-27-50(73)28-23-44)86-64(97)55(82-43(3)92)37-46-21-26-48-15-7-8-16-49(48)35-46/h7-8,11,14-16,21-31,35,40,42,52-60,91,93H,5-6,9-10,12-13,17-20,32-34,36-39,41H2,1-4H3,(H2,74,94)(H,81,100)(H,82,92)(H,83,95)(H,84,101)(H,85,96)(H,86,97)(H,87,98)(H,88,99)(H4,75,76,79)(H3,77,80,104)/t42-,52+,53-,54+,55-,56-,57-,58+,59+,60+/m1/s1

InChI Key

KATZUZNTRINHDT-HALMFYTRSA-N

Canonical SMILES

CCCCC(C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)NC(C)C(=O)N)NC(=O)C(CCCCNC(=O)N)NC(=O)C(CC2=CC=C(C=C2)O)N(C)C(=O)C(CO)NC(=O)C(CC3=CN=CC=C3)NC(=O)C(CC4=CC=C(C=C4)Cl)NC(=O)C(CC5=CC6=CC=CC=C6C=C5)NC(=O)C

1.Ozarelix, a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors.

Festuccia C1, Dondi D, Piccolella M, Locatelli A, Gravina GL, Tombolini V, Motta M. Prostate. 2010 Sep 1;70(12):1340-9. doi: 10.1002/pros.21169.

BACKGROUND AND AIMS: Antagonistic or agonistic analogues of gonadotropin-releasing hormone are extensively used for the treatment of advanced hormone-dependent prostate cancer. However, the majority of recurrent prostate tumors is androgen independent. This study explored the in vitro effects on DU145 and PC3 cell lines, two models of androgen-independent prostate cancer, of a fourth generation GnRH antagonist (Ozarelix).

2.Fluorescence spectroscopic determination of the critical aggregation concentration of the GnRH antagonists Cetrorelix, Teverelix and Ozarelix.

Schneider A1, Lang A, Naumann W. J Fluoresc. 2010 Nov;20(6):1233-40. doi: 10.1007/s10895-010-0674-5. Epub 2010 Jun 1.

The fluorescence spectroscopic behavior of three 2-naphthylalanine containing Gonadotropin-releasing hormone (GnRH) antagonists Cetrorelix, Teverelix and Ozarelix has been investigated concerning their aggregation process in comparison to the non-aggregating peptide D-Phe(6)-GnRH. The aim of the present investigation consisted in developing a method to determine the critical aggregation concentration for these decapeptides. This was achieved by monitoring the incorporation of the fluorescent probe 1-anilino-8-naphthalene sulfonate (ANS) into aggregates and utilizing the modification of band shape and intensity of the intrinsic peptide fluorescence emission depending on the analyzed peptide concentrations. Finally an approach for the explanation of the observed band characteristics is presented analyzing the fluorescence of fragments Cetrorelix(1-4) and Cetrorelix(1-6).