1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Androgen Receptor 5 alpha Reductase
  3. MK-4541

MK-4541 是一种选择性、口服有效的雄激素受体 (AR) 调节剂。MK-4541 可作为拮抗剂抑制 5α-还原酶。MK-4541 抑制 AR 阳性前列腺癌细胞的增殖并诱导凋亡 (apoptosis)。MK-4541可显著抑制 R3327-G 前列腺肿瘤在异种移植小鼠模型中的生长。

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MK-4541 Chemical Structure

MK-4541 Chemical Structure

CAS No. : 796885-38-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model[1].

体内研究
(In Vivo)

MK-4541 (100 mg/kg; 每天1次,每周5次,持续5周) 抑制含 R-3327-G 细胞的无胸腺裸鼠前列腺肿瘤生长[1]
MK-4541 (100 mg/kg, 200 mg/kg; 每周5次,持续5周) 对精囊具有抗雄激素作用,降低完好男性的血浆睾酮浓度,并抑制 Ki67 表达[1]
MK-4541 (15 mg/kg, 50 mg/kg; 每周5次,持续8周) 导致成年阉割小鼠肌肉骨骼质量和功能的损失[1]

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

Animal Model: R3327-G prostate tumors in xenograft mouse model[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg
Administration: Oral gavage; once daily, 5 times per week for 5 weeks
Result: Significantly inhibited tumor growth at 100 mg/kg, as well as reducing plasma testosterone concentration and Ki67 expression.
分子量

428.49

Formula

C22H31F3N2O3

CAS 号
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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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • 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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产品名称:
MK-4541
目录号:
HY-125065
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