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.
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- Reinheit: 98.58%
- CAS. Nr.: 328947-93-9
- Formel: C14H9F9N2O
- Molecular Weight:392.22
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Speicherung:
-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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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.
Chemical Information
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CAS. Nr. 328947-93-9
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Appearance Solid
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Molecular Weight 392.22
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[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 Related Classifications
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