产品
编 号：F178242
分子式：C74H100ClN15O14
分子量：1459.13
分子式：C74H100ClN15O14
分子量：1459.13
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CAS No: 151272-78-5
产品详情
生物活性：
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer.
体内研究：
Teverelix (3-300 μg/kg, intramuscular injection) inhibits testosterone in rats.Teverelix (1 mg/kg, s.c, daily for 3 days) abolishes luteal function in stumptailed macaques.Animal Model:Rats
Dosage:300, 100, 30, 10 and 3 μg/kg
Administration:Intramuscular injection
Result:Showed dose-response and time-course of testosterone inhibitory activity.
体外研究：
Teverelix (10 nM, 45 mins) inhibits GnRH-induced intracellular Ca2+ increase in HEK293/GnRHR cells.Teverelix (0.1 nM-1 μM, 45 mins) inhibits GnRH-induced cAMP accumulation in HEK293/GnRHR cells.Teverelix (10 nM-1 μM, 15 mins) inhibits GnRH-induced pERK1/2 and pCREB activation in HEK293/GnRHR cells.Teverelix inhibits histamine release in a peritoneal rat mast cell, with an EC50value of 81 μg/mL.
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer.
体内研究：
Teverelix (3-300 μg/kg, intramuscular injection) inhibits testosterone in rats.Teverelix (1 mg/kg, s.c, daily for 3 days) abolishes luteal function in stumptailed macaques.Animal Model:Rats
Dosage:300, 100, 30, 10 and 3 μg/kg
Administration:Intramuscular injection
Result:Showed dose-response and time-course of testosterone inhibitory activity.
体外研究：
Teverelix (10 nM, 45 mins) inhibits GnRH-induced intracellular Ca2+ increase in HEK293/GnRHR cells.Teverelix (0.1 nM-1 μM, 45 mins) inhibits GnRH-induced cAMP accumulation in HEK293/GnRHR cells.Teverelix (10 nM-1 μM, 15 mins) inhibits GnRH-induced pERK1/2 and pCREB activation in HEK293/GnRHR cells.Teverelix inhibits histamine release in a peritoneal rat mast cell, with an EC50value of 81 μg/mL.
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