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Cetrorelix Acetate (SB-075 acetate) Sale

(Synonyms: 醋酸西曲瑞克; SB-75 acetate) 目录号 : GC33467

A synthetic peptide GnRHR antagonist

Cetrorelix Acetate (SB-075 acetate) Chemical Structure

Cas No.:145672-81-7

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1mg
¥491.00
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5mg
¥884.00
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10mg
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25mg
¥2,945.00
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50mg
¥4,284.00
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产品描述

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 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.

1.Beckers, T., Reil?nder, H., and Hilgard, P.Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assayAnal. Biochem.251(1)17-23(1997) 2.Yano, T., Pinski, J., Halmos, G., et al.Inhibition of growth of OV-1063 human epithelial ovarian cancer xenografts in nude mice by treatment with luteinizing hormone-releasing hormone antagonist SB-75Proc. Natl. Acad. Sci. USA91(15)7090-7094(1994) 3.Meirow, D., Assad, G., Dor, J., et al.The GnRH antagonist cetrorelix reduces cyclophosphamide-induced ovarian follicular destruction in miceHum. Reprod.19(6)1294-1299(2004)

Chemical Properties

Cas No. 145672-81-7 SDF
别名 醋酸西曲瑞克; SB-75 acetate
Canonical SMILES N-acetyl-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-Ser-Tyr-{Cit}-Leu-Arg-Pro-Ala-NH2
分子式 C72H96ClN17O16 分子量 1491.09
溶解度 DMSO : 50 mg/mL (33.53 mM) 储存条件 -20°C, protect from light
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1 mM 0.6707 mL 3.3533 mL 6.7065 mL
5 mM 0.1341 mL 0.6707 mL 1.3413 mL
10 mM 0.0671 mL 0.3353 mL 0.6707 mL
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Research Update

Extracellular matrix in uterine leiomyoma pathogenesis: a potential target for future therapeutics

Hum Reprod Update 2018 Jan 1;24(1):59-85.PMID:29186429DOI:10.1093/humupd/dmx032.

Background: Uterine leiomyoma (also known as fibroid or myoma) is the most common benign tumor of the uterus found in women of reproductive age. It is not usually fatal but can produce serious clinical symptoms, including excessive uterine bleeding, pelvic pain or pressure, infertility and pregnancy complications. Due to lack of effective medical treatments surgery has been a definitive choice for the management of this tumor. Objective and rationale: Extracellular matrix (ECM) accumulation and remodeling are thought to be crucial for fibrotic diseases such as uterine leiomyoma. Indeed, ECM plays important role in forming the bulk structure of leiomyoma, and the ECM-rich rigid structure within these tumors is thought to be a cause of abnormal bleeding and pelvic pain. Therefore, a better understanding of ECM accumulation and remodeling is critical for developing new therapeutics for uterine leiomyoma. Search methods: PubMed and Google Scholar were searched for all original and review articles/book chapters related to ECM and medical treatments of uterine leiomyoma published in English until May 2017. Outcomes: This review discusses the involvement of ECM in leiomyoma pathogenesis as well as current and future medical treatments that target ECM directly or indirectly. Uterine leiomyoma is characterized by elevated levels of collagens, fibronectin, laminins and proteoglycans. They can induce the mechanotransduction process, such as activation of the integrin-Rho/p38 MAPK/ERK pathway, resulting in cellular responses that are involved in pathogenesis and altered bidirectional signaling between leiomyoma cells and the ECM. ECM accumulation is affected by growth factors (TGF-β, activin-A and PDGF), cytokines (TNF-α), steroid hormones (estrogen and progesterone) and microRNAs (miR-29 family, miR-200c and miR-93/106b). Among these, TGF-βs (1 and 3) and activin-A have been suggested as key players in the accumulation of excessive ECM (fibrosis) in leiomyoma. The presence of elevated levels of ECM and myofibroblasts in leiomyoma supports the fibrotic character of these tumors. Interestingly, ECM may serve as a reservoir of profibrotic growth factors and enhance their activity by increasing their stability and extending their duration of signaling. At present, several classes of compounds, including gonadotropin-releasing hormone (GnRH) agonist (leuprolide acetate), GnRH antagonist (Cetrorelix Acetate), selective progesterone receptor modulators (ulipristate acetate and asoprisnil), antiprogestin (mifepristone) and natural compounds like vitamin D and resveratrol have been studied as medical treatments that target ECM in uterine leiomyoma. Wider implications: Although several types of drugs (mostly antiproliferative agents) are available for leiomyoma treatment, none of them were introduced specifically as antifibrotic agents. In light of its critical role in the process of fibrosis in leiomyoma, we propose that ECM should be considered as a crucial target for future therapeutics. Thus, the introduction of drugs that are specifically antifibrotic could be a good solution to control abnormal leiomyoma growth and associated clinical symptoms. The antifibrotic compounds can be introduced based on their ability to regulate ECM components and their receptors, as well as growth factors, cytokines, steroid hormones and their corresponding receptors and intracellular signaling pathways, as well as microRNAs, involved in ECM production in leiomyoma.

Identification and structural elucidation of a new cetrorelix methylene dimer impurity in Cetrorelix Acetate by using LC-MS/MS

J Pharm Biomed Anal 2021 Apr 15;197:113946.PMID:33611089DOI:10.1016/j.jpba.2021.113946.

Cetrorelix, a potent third generation of luteinizing hormone releasing hormone (LHRH) antagonist, is a synthetic decapeptide used for treatment of infertility, prostatic hypertrophy and sexual hormone-dependent tumors. The approved drug of cetrorelix (Cetrotide, Asta Medica AG, Frankfurt, Germany.), was used for prevention of premature ovulation in patients undergoing a controlled ovarian stimulation (COS), followed by oocyte pick-up and assisted reproductive techniques, and has been shown safe and effective in controlled ovarian stimulation. Nevertheless, the study of aggregation products of cetrorelix was rarely reported. A simple liquid chromatography mass spectrometry (LC-MS/MS) method was developed for separation, identification and characterization of a new cetrorelix methylene dimer impurity in cetrorelix. The chromatographic separation was achieved on an XSelect Peptide CSH ™C18 column (150 × 4.6 mm, 3.5 μm particle size) using gradient elution with a mobile phase of ammonium formate buffer (pH 3.0, 20 mM), acetonitrile at a flow rate 1.0 mL min-1, and an ultraviolet detection wavelength of 226 nm. The new cetrorelix methylene dimer impurity was characterized by LC-MS/MS and it characteristic fragment ions were summarized. A simple, fast and accurate method was established for the determination of the molecular weight and structure of the new cetrorelix methylene dimer impurity. In this study, the results showed that the cetrorelix was highly unstable in formaldehyde conditions. In addition, it is proposed that the impact of formaldehyde in the environment on the quality of Cetrorelix Acetate for Injection should be evaluated during the production process.

Delivery of Peptidic Gonadotropin Releasing Hormone Antagonists

Curr Drug Deliv 2018;15(5):602-609.PMID:29446744DOI:10.2174/1567201815666180214142300.

GnRH antagonists have several clinical applications in prostate cancer, regulation of ovulation induction in females, breast cancer, male contraception and others. Antagonists differ from natural GnRH decapeptide in having five or more amino acid substitutions, whereas most of the antagonists are available as subcutaneous (SC) formula for injection some are formulated as a depot formulation for sustained release (e.g., Cetrorelix, Degarelix). Systemic delivery of Cetrorelix Acetate by intratracheal route can be achieved using dry powder for inhalation of the adhesive mixture when the powder deposition reaches stage four. The oral route for systemic delivery of peptide without its degradation can be achieved using gastrointestinal permeation enhancement technology GIPET® provided by acyline.

Therapeutic effects of an oral gonadotropin-releasing hormone receptor antagonist, relugolix, on preventing premature ovulation in mild ovarian stimulation for IVF

Reprod Med Biol 2021 Oct 19;21(1):e12422.PMID:34938146DOI:10.1002/rmb2.12422.

Purpose: Can relugolix, a novel oral gonadotropin-releasing hormone receptor (GnRH) antagonist, function as an alternative ovulation inhibitor to GnRH antagonist injections? Methods: This single-center, cross-sectional retrospective study compared premature ovulation rates and clinical outcomes in IVF treatment after mild ovarian stimulation with 40 mg of relugolix (relugolix group) or 0.25-mg injections of ganirelix acetate or Cetrorelix Acetate (injection group) between March 2019 and January 2020. Of 247 infertile women (256 IVF cycles) aged ≤42 years, 223 women (230 cycles) were evaluated. In the relugolix and injection groups, we compared 104 and 85 cycles after GnRH antagonist use before the LH surge (LH levels <10 mIU/ml) and 22 and 19 cycles during the LH surge (LH levels ≥10 mIU/ml), respectively. Results: Before the LH surge, the ovulation rates in the two groups were very low (p = 0.838), however; during the LH surge, the cycles using relugolix had a high ovulation rate of 40.9% compared with no ovulation in the injection group (p = 0.002). There were no significant differences in embryo culture findings and pregnancy outcomes between the two groups. Conclusions: Although relugolix had a high ovulation suppressive effect, when the LH surge occurred, its effect was insufficient.

Efficacy and Safety of gonadotropin-releasing hormone (GnRH) Agonists Triptorelin Acetate and Cetrorelix Acetate in Assisted Reproduction

Med Sci Monit 2018 Nov 8;24:7996-8000.PMID:30405094DOI:10.12659/MSM.911345.

BACKGROUND The aim of this study was to compare the efficacy and safety of 2 GnRH agonists - triptorelin acetate and Cetrorelix Acetate - in assisted reproduction. MATERIAL AND METHODS A total of 182 females who received in vitro fertilization and embryo transfer (IVF+ET) from March 2014 to July 2014 were involved, and their clinical data were retrospectively analyzed. Among them, 91 patients received treatment with short-acting triptorelin (group A) and another 91 patients were treated with Cetrorelix Acetate (group B). Fasting blood was extracted from each patient on the day of administration of human chorionic gonadotropin (hCG), and serum levels of luteinizing hormone (LH), estradiol (E2), and progesterone (P) were detected using chemiluminescence method. The number of oocytes, fertilization rate, cleavage rate, and number of obtained embryos were recorded and compared. Pregnancy outcomes and adverse events were observed and compared. Expression level of FSH receptor (FSHR) in endometrial tissues was measured by qRT-PCR. RESULTS Serum level of E2 was significantly lower in group B than in group A (p<0.05). Indices, including the number of oocytes, fertilization rate and cleavage rate, number of obtained embryos, and pregnancy rate, were slightly better in group B than in group A, but no significant differences were found. The incidence of ovarian hyperstimulation syndrome (OHSS) was significant higher in group A than in group B (p<0.05). FSHR expression level was significantly lower in group B than in group A. CONCLUSIONS The effect of Cetrorelix Acetate is superior to that of short-acting triptorelin in assisted reproduction. Our most important finding is that Cetrorelix Acetate reduced the incidence of OHSS.