LGD-2226
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.58%
- CAS 番号: 328947-93-9
- 分子式: C14H9F9N2O
- 分子量:392.22
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
EC50: 0.2 nM (Androgen receptor)[1]; Ki: 1.5 nM (Androgen receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
0.2 nM
Compound: 4m, LGD2226
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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
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[PMID: 17034117] |
| CV-1 | IC50 |
>10000 nM
Compound: 4m, LGD2226
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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
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[PMID: 17034117] |
| CV-1 | EC50 |
0.2 nM
Compound: 13i
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Agonist activity at human androgen receptor expressed in CV1 cells
Agonist activity at human androgen receptor expressed in CV1 cells
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[PMID: 17257838] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult orchidectomized (ORDX) rats[1]
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Dosage:1-100 mg/kg
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Administration:Oral administration; daily; for 2 weeks
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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.
化学情報
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CAS 番号 328947-93-9
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性状 Solid
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分子量 392.22
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分子式 C14H9F9N2O
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Color Light yellow to green yellow
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SMILES
O=C1NC2=C(C=C(N(CC(F)(F)F)CC(F)(F)F)C=C2)C(C(F)(F)F)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. van Oeveren A, et al. Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator. J Med Chem. 2006 Oct 19;49(21):6143-6. [Content Brief]
[2]. Miner JN, et al. An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate. Endocrinology. 2007 Jan;148(1):363-73. [Content Brief]
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 |
LGD-2226 関連分類
HY-105318 関連分類
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