Cetrorelix Acetate
Based on 2 publication(s) in Google Scholar
Cetrorelix (SB-75) acetate is a competitive gonadotropin-releasing hormone receptor (GnRHR) antagonist with a Kd of 0.19 nM. Cetrorelix acetate inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby suppressing the secretion of downstream sex steroids. Cetrorelix acetate prevents ovulation, induces reversible reproductive shutdown and azoospermia, reduces ovarian fibrosis, improves superovulation outcomes, and inhibits chemotherapy-induced mitochondria-dependent apoptosis. Cetrorelix acetate is applicable for fertility assistance research.
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- 純度: 99.98%
- CAS 番号: 145672-81-7
- 分子式: C72H96ClN17O16
- 分子量:1491.09
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保管条件:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Cetrorelix acetate
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生物活性
製品説明
体外実験
Cetrorelix acetate induces minimal histamine release from rat mast cells, with an ED50 far above pharmacologically relevant plasma concentrations[3].
Cetrorelix acetate 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.
体内実験
Cetrorelix (5 μg/day; i.p.; daily; 20 days) acetate alone has no detectable effect on ovarian granulosa cell apoptosis, hormone levels, or mitochondrial function in healthy female Sprague-Dawley rats[1].
Cetrorelix (5 µg/kg; i.p.; once every 3 days or daily; 1 week) acetate significantly increases the number of normal superovulated oocytes in aged female C57BL/6J mice (to 9.8 and 8.7 oocytes, respectively) acetate, reduces ovarian fibrosis, and maintains normal oocyte fertilization and fetal development rates[2].
Cetrorelix (~10 μg/kg; s.c.; single dose) acetate 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) acetate 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.
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Animal Model:Sprague-Dawley (female, 250 g)[1]
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Dosage:5 μg/day (pretreatment); 5 μg/day + 20 mg/kg/day (combined with alkylating antineoplastic agent)
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Administration:i.p.; daily; 10 days (pretreatment); i.p.; daily; 10 days (combined)
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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%.
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Animal Model:Sprague-Dawley (female, 250 g)[1]
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Dosage:5 μg/day
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Administration:i.p.; daily; 20 days
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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.
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Animal Model:C57BL/6J (female, 52 weeks old, aged)[2]
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Dosage:5 µg/kg (3 doses over 1 week); 5 µg/kg (7 doses over 1 week)
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Administration:i.p.; once every 3 days (3 doses over 1 week); daily (7 doses over 1 week)
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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.
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Animal Model:Male castrated rats[3]
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Dosage:2.5 μg/rat (~10 μg/kg)
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Administration:s.c.; single dose
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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.
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Animal Model:Male castrated cynomolgus monkeys (*Macaca fascicularis*)[3]
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Dosage:250 μg/kg; 625 μg/kg; 1250 μg/kg
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Administration:s.c.; single dose
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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.
化学情報
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CAS 番号 145672-81-7
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性状 Solid
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分子量 1491.09
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分子式 C72H96ClN17O16
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Color White to off-white
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別名
SB-75 acetate; 酢酸セトロレリックス
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配列
N-acetyl-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-Ser-Tyr-{Cit}-Leu-Arg-Pro-Ala-NH2
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シーケンスの短縮
Ac-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-SY-{Cit}-LRPA-NH2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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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
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (33.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (1.34 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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参考文献
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.6707 mL | 3.3533 mL | 6.7065 mL | 16.7663 mL |
| DMSO | 5 mM | 0.1341 mL | 0.6707 mL | 1.3413 mL | 3.3533 mL |
| 10 mM | 0.0671 mL | 0.3353 mL | 0.6707 mL | 1.6766 mL | |
| 15 mM | 0.0447 mL | 0.2236 mL | 0.4471 mL | 1.1178 mL | |
| 20 mM | 0.0335 mL | 0.1677 mL | 0.3353 mL | 0.8383 mL | |
| 25 mM | 0.0268 mL | 0.1341 mL | 0.2683 mL | 0.6707 mL | |
| 30 mM | 0.0224 mL | 0.1118 mL | 0.2236 mL | 0.5589 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Cetrorelix acetate 関連分類
HY-P0009A 関連分類
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