2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. LGD-2226

LGD-2226 是一种选择性和口服活性的雄激素受体 (AR) 调节剂，对人雄激素受体的 EC50 为 0.2 nM，Ki 为 1.5 nM。LGD-2226 在动物模型中显示出组织选择性，与肌肉相比，对前列腺的作用较低。LGD-2226 可用于肌肉萎缩，骨质疏松和性功能障碍的研究。

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LGD-2226 Chemical Structure

LGD-2226 Chemical Structure

CAS No. : 328947-93-9

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Customer Review

LGD-2226 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

LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction[1][2].

IC50 & Target

EC50: 0.2 nM (Androgen receptor)[1]; Ki: 1.5 nM (Androgen receptor)[1]
体外研究
(In Vitro)

LGD-2226 (Compound 4m) occupies the same binding pocket as dihydrotestosterone (DHT), and in general, the protein backbone is superposable to that observed with DHT. Just like the carbonyl group of DHT, the quinolone carbonyl forms hydrogen bond interactions with GLN711 and ARG752. GLN711 forms an additional hydrogen bond with the quinolone NH of LGD-2226. The trifluoroethyl groups of LGD-2226 occupy the same space in the receptor as the C and D rings of the steroid[1].

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

LGD-2226 相关抗体:
体内研究
(In Vivo)

LGD-2226 (Compound 4m; 1-100 mg/kg; oral administration; daily; for 2 weeks; adult oORDX rats) has a pronounced effect on the levator ani muscle, maintaining the muscle weight at the eugonadal levels at an approximate 3 mg/kg dose. LGD-2226 has weak trophic effects on the prostate. An amount of 100 mg/kg LGD-2226 is required to maintain prostate weight at intact levels. These data clearly show the tissue selectivity of LGD-2226[1].

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

Animal Model: Adult orchidectomized (ORDX) rats[1]
Dosage: 1-100 mg/kg
Administration: Oral administration; daily; for 2 weeks
Result: Had a pronounced effect on the levator ani muscle, maintaining the muscle weight at the eugonadal levels at an approximate 3 mg/kg dose.
分子量

392.22

Formula

C14H9F9N2O
CAS 号
性状

固体

颜色

Light yellow to green yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (318.70 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5496 mL 12.7479 mL 25.4959 mL
5 mM 0.5099 mL 2.5496 mL 5.0992 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

LGD-2226 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5496 mL 12.7479 mL 25.4959 mL 63.7397 mL
5 mM 0.5099 mL 2.5496 mL 5.0992 mL 12.7479 mL
10 mM 0.2550 mL 1.2748 mL 2.5496 mL 6.3740 mL
15 mM 0.1700 mL 0.8499 mL 1.6997 mL 4.2493 mL
20 mM 0.1275 mL 0.6374 mL 1.2748 mL 3.1870 mL
25 mM 0.1020 mL 0.5099 mL 1.0198 mL 2.5496 mL
30 mM 0.0850 mL 0.4249 mL 0.8499 mL 2.1247 mL
40 mM 0.0637 mL 0.3187 mL 0.6374 mL 1.5935 mL
50 mM 0.0510 mL 0.2550 mL 0.5099 mL 1.2748 mL
60 mM 0.0425 mL 0.2125 mL 0.4249 mL 1.0623 mL
80 mM 0.0319 mL 0.1593 mL 0.3187 mL 0.7967 mL
100 mM 0.0255 mL 0.1275 mL 0.2550 mL 0.6374 mL
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:

LGD-2226328947-93-9LGD2226LGD 2226Androgen ReceptorDihydrotestosteroneorally levatoranimuscletissueselectivitynonsteroidalGLN711wastingosteoporosisInhibitorinhibitorinhibit

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目录号：
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