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Cetrorelix diacetate

Name: Cetrorelix diacetate
Brand: MedChemExpress
SKU: HY-P0009B
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(Synonyms: SB-75 diacetate)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Cetrorelix (SB-75) diacetate is a competitive gonadotropin-releasing hormone receptor (GnRHR) antagonist with a K_d of 0.19 nM. Cetrorelix diacetate inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby suppressing the secretion of downstream sex steroids. Cetrorelix diacetate prevents ovulation, induces reversible reproductive shutdown and azoospermia, reduces ovarian fibrosis, improves superovulation outcomes, and inhibits chemotherapy-induced mitochondria-dependent apoptosis. Cetrorelix diacetate is applicable for fertility assistance research.

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CAS No.: 130143-01-0
Formule: C₇₄H₁₀₀ClN₁₇O₁₈
Masse moléculaire:1551.14

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Cetrorelix diacetate Chemical Structure

CAS No.: 130143-01-0

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

In Vitro

Cetrorelix induces minimal histamine release from rat mast cells, with an ED₅₀ far above pharmacologically relevant plasma concentrations^[3].
Cetrorelix does not inhibit EGF-stimulated proliferation of human granulosa cells at pharmacologically relevant concentrations, with inhibitory effects only seen at ~100-fold higher concentrations^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ApoptosisMitochondrial FunctionOthers

Apoptosis

Mitochondrial Function

Cetrorelix (5 μg/day; i.p.; daily; 20 days total) pretreatment inhibits alkylating antineoplastic agent-induced ovarian granulosa cell apoptosis via suppression of mitochondria-dependent apoptotic pathways, and restoring normal serum estradiol levels and mitochondrial function^[1].
Cetrorelix (5 μg/day; i.p.; daily; 20 days) alone has no detectable effect on ovarian granulosa cell apoptosis, hormone levels, or mitochondrial function in healthy female Sprague-Dawley rats^[1].

Others

Cetrorelix (5 µg/kg; i.p.; once every 3 days or daily; 1 week) significantly increases the number of normal superovulated oocytes in aged female C57BL/6J mice (to 9.8 and 8.7 oocytes, respectively), reduces ovarian fibrosis, and maintains normal oocyte fertilization and fetal development rates^[2].
Cetrorelix (~10 μg/kg; s.c.; single dose) immediately suppresses plasma LH by >80% in male castrated rats, with full recovery within 24 hours^[3].
Cetrorelix (250-1250 μg/kg; s.c.; single dose) immediately suppresses LH in male castrated cynomolgus monkeys, with suppression lasting for at least 96 hours^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (female, 250 g)^[1]
Dosage:

5 μg/day (pretreatment); 5 μg/day + 20 mg/kg/day (combined with alkylating antineoplastic agent)
Administration:

i.p.; daily; 10 days (pretreatment); i.p.; daily; 10 days (combined)
Result:

Reduced granulosa cell apoptotic index from 13.6% to 3.1%.
Restored serum estradiol levels from ~80 pg/mL to ~160 pg/mL.
Preserved normal granulosa cell ultrastructure including intact mitochondria.
Reversed alkylating antineoplastic agent-induced mitochondrial depolarization, resulting in a green fluorescence intensity of 15.36, red fluorescence intensity of 23.16, and a red/green ratio of 1.51.
Inhibited alkylating antineoplastic agent-induced cytochrome c release from mitochondria to cytoplasm.
Suppressed alkylating antineoplastic agent-induced increases in Bax-positive cells from 90% to 25%, caspase-3-positive cells from 85% to 30%, and cytochrome c-positive cells from 80% to 30%.
Restored alkylating antineoplastic agent-reduced Bcl-2-positive cells from 40% to 70%.

Animal Model:

Sprague-Dawley (female, 250 g)^[1]
Dosage:

5 μg/day
Administration:

i.p.; daily; 20 days
Result:

Did not alter granulosa cell apoptotic index (2.8%, similar to control's 2.5%).
Did not change serum estradiol or progesterone levels.
Did not affect granulosa cell ultrastructure, mitochondrial membrane potential, cytochrome c distribution between mitochondria and cytoplasm, or expression levels of Bax, Bcl-2, caspase-3, or cytochrome c.

Animal Model:

C57BL/6J (female, 52 weeks old, aged)^[2]
Dosage:

5 µg/kg (3 doses over 1 week); 5 µg/kg (7 doses over 1 week)
Administration:

i.p.; once every 3 days (3 doses over 1 week); daily (7 doses over 1 week)
Result:

Increased mean total oocyte count to 13.2 (3-dose group) and 11.4 (7-dose group), with normal oocyte counts increased to 9.8 (74.2% normal rate) and 8.7 (76.3% normal rate), respectively, compared to controls (P<0.05).
Achieved fertilization rates of 96.9% (3-dose group) and 88.5% (7-dose group), with birth rates of 58.3% and 51.8%, respectively, comparable to control values.
Reduced ovarian fibrosis, with phalloidin-positive area percentage decreased compared to untreated aged controls (P<0.05).
Showed no significant difference in ovary weight compared to control aged mice.

Animal Model:

Male castrated rats^[3]
Dosage:

2.5 μg/rat (~10 μg/kg)
Administration:

s.c.; single dose
Result:

Suppressed plasma LH concentrations immediately, reaching a nadir at 4 hours with an >80% fall in LH concentrations.
Returned serum LH to normal levels within 24 hours.

Animal Model:

Male castrated cynomolgus monkeys (*Macaca fascicularis*)^[3]
Dosage:

250 μg/kg; 625 μg/kg; 1250 μg/kg
Administration:

s.c.; single dose
Result:

Suppressed LH concentrations immediately across all doses, reaching a nadir at ~12 hours post-injection.
Maintained LH concentrations suppressed for at least 96 hours.
Showed no LH rebound within the 96-hour interval at any dose.

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Chemical Information

CAS No. 130143-01-0
Masse moléculaire 1551.14
Formule C₇₄H₁₀₀ClN₁₇O₁₈
Synonyms

SB-75 diacetate
Sequence Shortening

Ac-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-SY-{Cit}-LRPA-NH2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

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Journal Impact Factor

Commun Biol

Diurnal testosterone oscillations gate drug delivery via phase separation of ZO-1 at the blood-testis barrier in mice. [Abstract]

2026 Jun 1. PMID: 42219451
Gen Comp Endocrinol

Neuromodulatory effects of GnRH on the caudal neurosecretory Dahlgren cells in female olive flounder. [Abstract]

2021 Jun 1:307:113754. PMID: 33711313

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (291 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Zhao XJ, et al. GnRH antagonist cetrorelix inhibits mitochondria-dependent apoptosis triggered by chemotherapy in granulosa cells of rats. Gynecologic oncology. 2010 Jul;118(1):69-75. [Content Brief]

[2]. Kanda A, et al. Effect of Cetrorelix administration on ovarian stimulation in aged mice. Experimental animals. 2021 Feb 06;70(1):31-36. [Content Brief]

[3]. Reissmann T, et al. The LHRH antagonist cetrorelix: a review. Human reproduction update. 2000;6(4):322-31. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Cetrorelix diacetate

2 Cited Publications

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Cetrorelix diacetate

Publications Citing Use of MedChemExpress (MCE) Cetrorelix diacetate