Teverelix

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Teverelix

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

151272-78-5

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

EP 24332

产品介绍

Teverelix (EP 24332) 是一种GnRH拮抗剂。Teverelix 可竞争性和可逆性地与 GnRH 受体 (GnRH receptors)结合，从而抑制 LH 和 FSH 的释放。Teverelix 可用于前列腺增生、子宫内膜异位症和前列腺癌的研究。

生物活性

Teverelix (EP 24332) is aGnRHantagonist. Teverelix binds competitively and reversibly toGnRH receptors, thereby suppressing the release of LH andFSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostatecancer^[1]^[2].

体外研究
(In Vitro)

Teverelix (10 nM, 45 mins) inhibits GnRH-induced intracellular Ca²⁺increase in HEK293/GnRHR cells^[2].
Teverelix (0.1 nM-1 μM, 45 mins) inhibits GnRH-induced cAMP accumulation in HEK293/GnRHR cells^[2].
Teverelix (10 nM-1 μM, 15 mins) inhibits GnRH-induced pERK1/2 and pCREB activation in HEK293/GnRHR cells^[2].
Teverelix inhibits histamine release in a peritoneal rat mast cell, with an EC₅₀value of 81 μg/mL^[3].

Western Blot Analysis^[2]

Cell Line:	HEK293/GnRHR cells
Concentration:	10 nM, 100 nM, 1 μM
Incubation Time:	15 mins
Result:	Inhibited GnRH-induced pERK1/2 and pCREB activation.

体内研究
(In Vivo)

Teverelix (3-300 μg/kg, intramuscular injection) inhibits testosterone in rats^[3].
Teverelix (1 mg/kg, s.c, daily for 3 days) abolishes luteal function in stumptailed macaques^[4].

Animal Model:	Rats^[3]
Dosage:	300, 100, 30, 10 and 3 μg/kg
Administration:	Intramuscular injection
Result:	Showed dose-response and time-course of testosterone inhibitory activity.

Clinical Trial

分子量

1459.13

Formula

C₇₄H₁₀₀ClN₁₅O₁₄

CAS 号

151272-78-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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