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  3. Tan-931

Tan-931 是一种非竞争性的选择性芳香化酶 (aromatase) 抑制剂,对 aromataseIC50 为 17.2 μM,对 human aromataseKi 为 40 μM,对 rat aromataseIC50 为 162 μM。Tan-931 降低 PMSG (HY-N12634) 处理的雌性大鼠血浆雌二醇 -17β 水平以及卵巢和子宫重量。Tan-931 可用于雌激素依赖性转移性乳腺癌的研究。

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Tan-931

Tan-931 Chemical Structure

CAS No. : 127448-92-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tan-931 is a non-competitive and selective inhibitor of aromatase , with an IC50 is 17.2 μM and a Ki of 40 μM for human aromatase, and an IC50 of 162 μM for rat aromatase. Tan-931 reduces plasma estradiol-17β level and weight of ovaries and uterus in PMSG (HY-N12634)-treated female rats. Tan-931 can be used for the research of estrogen-dependent metastatic breast cancer[1][2].

IC50 & Target[1][2]

Aromatase

17.2 μM (IC50)

Aromatase

40 μM (Ki)

体外研究
(In Vitro)

Tan-931 在微粒体测定中对芳香化酶的抑制作用较弱,其 IC50 为 17.2 μM[2]。

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

体内研究
(In Vivo)

Tan-931 (25-100 mg/kg;皮下注射;每日给药持续 4 天) 降低 PMSG 处理的雌性大鼠血浆雌二醇 17β 水平以及卵巢和子宫的重量 [1].
Tan-931 (100 mg/kg;皮下注射;每天给药 2 次持续 7 天) 未引起大鼠肾上腺肥大[1].

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

Animal Model: Female Sprague-Dawley (20-day-old) challenged with PMSG[1]
Dosage: 25, 50, 100 mg/kg
Administration: s.c.; daily for 4 days
Result: Reduced PMSG-induced increases in plasma estradiol-17β level and ovarian weight in a dose-dependent manner.
Reduced plasma estradiol-17β.
Slightly reduced uterine weight.
Reduced total and specific ovarian aromatase activity.
Animal Model: Sprague-Dawley (9-week-old male)[1]
Dosage: 100 mg/kg
Administration: s.c., twice daily for 7 days
Result: Did not induce adrenal hypertrophy.
Caused a significant increase in body weight.
Did not affect liver weight relative to controls.
分子量

302.24

Formula

C15H10O7

CAS 号
结构分类
初始来源

Penicillium funiculosum

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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-180420
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