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  • Aminoglutethimide
    • 氨鲁米特;DL-Aminoglutethimide
    货号: abs813975
    CAS号: 125-84-8
    分子式: C13H16N2O2
    分子量: 232.28
    产品说明书
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    货号-规格 货期 价格 数量
    abs813975-25mg 1-2周 ¥432.00
    - +
    abs813975-50mg 1-2周 ¥775.00
    - +
    abs813975-100mg 1-2周 ¥930.00
    - +
    abs813975-200mg 1-2周 ¥1211.00
    - +
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    产品描述
    描述

    Aminoglutethimide 是一种芳香化酶抑制剂,IC50为10 μM。在体外人类胎盘芳香酶实验中,Aminoglutethimide 抑制芳香酶, IC50 为10 μM,这种酶在雄激素转化为雌激素的过程中涉及,且是乳腺癌的内分泌治疗中的一个重要靶点。 Aminoglutethimide作用于绵羊肾上腺皮质细胞,抑制ACTH 受体(ACTH-R) mRNA 表达,这种作用存在时间依赖性。Aminoglutethimide 作用于表达功能性 ACTH受体,产生糖皮质激素,盐皮质激素和雄激素的类固醇通路的人类NCI-h295 肾上腺皮质癌细胞系,通过影响基因表达,或者通过作用于RNA稳定性降低转录累积,显著抑制类固醇激素分泌和ACTH-R mRNA表达,这种作用存在剂量依赖性。

    纯度
    >98%
    储存/保存方法
    -20°C
    基本信息
    别名
    氨鲁米特;DL-Aminoglutethimide
    外观
    白色结晶性粉末
    可溶性/溶解性
    Ethanol :7 mg/mL (30.13 mM)

    DMSO :16 mg/mL (68.9 mM)
    生物活性
    靶点
    Aromatase
    In vitro(体外研究)
    Aminoglutethimide displays aromatase inhibition in vitro assay with human placental aromatase, which is an enzyme involved in the conversion of androgens into estrogens, and an important target for the endocrine treatment of breast cancer. Aminoglutethimide inhibits ACTH receptor (ACTH-R) mRNA expression in ovine adrenocortical cells in a time-dependent fashion. Aminoglutethimide significantly suppresses steroid secretion and the baseline ACTH-R mRNA expression in a dose-dependent fashion (300 μM AG, 5±1%; 30 μM AG, 64±1%; 3 μM AG, 108±19% compared with control cells, 100±11%) by affecting the gene expression or by decreasing transcript accumulation via an effect on RNA stability, in the human NCI-h295 adrenocortical carcinoma cell line, which expresses functional ACTH receptors and produces steroids of the glucocorticoid, mineralocorticoid and androgen pathway. Aminoglutethimide inhibits aromatase in a dose-dependent fashion with IC50 of 13 μM in 6 breast tumor homogenates, placental aromatase with IC50 of 6 μM and hypothalamic aromatase with IC50 of 8 μM.
    In vivo(体内研究)
    Aminoglutethimide accelerates its own metabolism from a basal value of 2.6±0.3 (S.E.) liters/24 hours to 5.3±1.4 liters/24 hours after 1 to 2 weeks of Aminoglutethimide administration, and markedly accelerates the metabolism of the synthetic glucocorticoid and dexamethasone, from basal values of 145±26.6 liters/24 hours to 568±127 liters/24 hours (p Aminoglutethimide (150 mg/kg) abolishes the induction of ornithine decarboxylase (ODC) and almost depletes the gonads and plasma of progesterone or testosterone elicited by human chorionic gonadotropin (hCG) in the ovary of adult female mice and the testis of immature male mice, which is related to an inhibition of cAMP-dependent protein kinase (IC50 287 μM) rather than blockade of the steroidogenic pathway.
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