2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. YM580

YM580 是一种强效、口服有效且选择性高的雄激素受体 (AR) 拮抗剂 (IC50 = 0.11 μM，hAR Ki = 4.6 nM，rAR Ki = 6.2 nM)。YM580 对 PR、GR 和 ERα 具有良好的选择性 (Ki > 3300 nM)。YM580 在成年完整大鼠中呈剂量依赖性地降低腹侧前列腺重量，且不影响血清睾酮水平。YM580 可用于前列腺癌的研究。

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YM580

YM580 Chemical Structure

CAS No. : 262295-11-4

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YM580 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC50 = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (Kis > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer[1].

IC50 & TargetAndrogen Receptor

hAR

4.6 nM (Ki)

rAR

6.2 nM (Ki)

rat PR

3300 nM (Ki)

human GR

>100000 nM (Ki)

human ERα

>100000 nM (Ki)

体外研究
(In Vitro)

YM580 在 AR/CHO#3 细胞中强力抑制 AR 介导的转录激活，其 IC50 为 0.11 μM[1]。

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

YM580 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value Note
Rat[1] 3 nM p.o. Cmax 702 ng/mL plasma
Rat[1] 3 nM p.o. AUC0-t 21952 ng·h/mL plasma
Rat[1] 3 nM p.o. T1/2 12.5 h plasma
Rat[1] 3 nM p.o. CL 133 mL/h/kg plasma
Rat[1] 3 nM p.o. Cmax 1561 ng/mL prostate
Rat[1] 3 nM p.o. AUC0-t 43215 h·ng/g prostate
Rat[1] 3 nM p.o. T1/2 11.2 h prostate
Rat[1] 3 nM p.o. CL 68.3 mL/h/kg prostate
体内研究
(In Vivo)

YM580 (0.3-30 mg/kg；口服；每日；连续 15 天) 可降低成熟完整雄性 Wistar 大鼠的腹侧前列腺重量，并表现出抗雄激素作用[1]。

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

Animal Model: Mature intact male Wistar rats (10-week-old)[1]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: p.o.; daily; 15 days
Result: Decreased ventral prostate weight in a dose-dependent manner with an ED50 of 2.2 mg/kg/day, and an inhibition rate of 67% at 10 mg/kg/day.
Exerted a maximum antiandrogenic effect comparable to surgical castration at 30 mg/kg/day.
Did not significantly elevate serum testosterone levels across all doses.
Exhibited good peripheral selectivity.
分子量

471.41

Formula

C21H19F6N5O
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

YM580 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

YM580262295-11-4YM 580YM-580Androgen ReceptorARestrogen receptors αprogesterone receptorsventral prostatemature intact ratsWistar ratsAR/CHO#3 cellsprostate cancerglucocorticoid receptorsInhibitorinhibitorinhibit

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YM580
目录号：
HY-180409
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