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

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.

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LGD-2226

LGD-2226 構造式

CAS 番号 : 328947-93-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 192 在庫あり
Solution
10 mM * 1 mL in DMSO USD 192 在庫あり
Solid
1 mg $60 在庫あり
5 mg $175 在庫あり
10 mg $305 在庫あり
25 mg $680 在庫あり
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Other Forms of LGD-2226:

LGD-2226 関連抗体

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製品説明

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]
Cellular Effect
Cell Line Type Value Description References
CV-1 EC50
0.2 nM
Compound: 13i
Agonist activity at human androgen receptor expressed in CV1 cells
Agonist activity at human androgen receptor expressed in CV1 cells
[PMID: 17257838]
CV-1 EC50
0.2 nM
Compound: 4m, LGD2226
Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay
Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay
[PMID: 17034117]
CV-1 IC50
> 10000 nM
Compound: 4m, LGD2226
Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay
Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay
[PMID: 17034117]
体外実験

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].

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

LGD-2226 関連抗体
体内実験

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].

MedChemExpress (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

分子式

C14H9F9N2O
CAS 番号
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1NC2=C(C=C(N(CC(F)(F)F)CC(F)(F)F)C=C2)C(C(F)(F)F)=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

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

DMSO : 125 mg/mL (318.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2550 mL 1.2748 mL 2.5496 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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純度とドキュメンテーション

純度: 98.58%

COA (253 KB) HNMR (259 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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LGD-2226 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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:

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

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製品名:
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製品番号:
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