LGD-2226 Overview
LGD-2226 is a synthetic, nonsteroidal small-molecule selective androgen receptor modulator (SARM) originally developed by Ligand Pharmaceuticals in collaboration with researchers at the University of Tennessee. It is part of the 6-alkylamino-2-quinolinone SARM structural class and is widely cited in the primary literature as a high-affinity, highly selective androgen receptor ligand. Reported binding studies describe a K_i of approximately 1 nM at the androgen receptor with >1,000-fold selectivity over the glucocorticoid, progesterone, mineralocorticoid, and estrogen receptors.
LGD-2226 is referenced in androgen receptor pharmacology research, SARM structure-activity studies, and analytical reference-standard work, including LC-MS/MS panels for SARM detection in anti-doping analytical literature.
Chemical Structure & Identification
- Chemical Name: 6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1H-quinolin-2-one
- Synonyms: LGD2226; LGD 2226
- CAS Number: 328947-93-9
- Molecular Formula: C₁₄H₉F₉N₂O
- Molecular Weight: 392.23 g/mol
- Appearance: Pale yellow to light yellow solid
- UNII: RI376RM5MT (FDA Unique Ingredient Identifier)
Structural Description: LGD-2226 is built on a 1H-quinolin-2-one (2-quinolinone) bicyclic scaffold, with a 4-trifluoromethyl substituent and a 6-position bis(2,2,2-trifluoroethyl)amino group. The molecule contains nine fluorine atoms distributed across three trifluoromethyl/trifluoroethyl groups, which contribute substantial electron-withdrawing character and influence the compound’s receptor binding affinity, metabolic stability, and lipophilicity. Structural identification and molecular data are referenced against PubChem and the FDA UNII database.
Mechanism of Action
LGD-2226 binds the androgen receptor ligand-binding domain with high affinity and acts as a selective agonist. Published binding studies report a unique pattern of androgen receptor protein-protein interactions distinct from those induced by testosterone or steroidal androgens, suggesting LGD-2226 induces a characteristic ligand-binding domain conformation upon receptor binding.
Reported in vitro and preclinical characterizations include:
- Androgen receptor binding K_i ≈ 1 nM
-
1,000-fold selectivity over GR, PR, MR, and ER
- Differential transcriptional output observed in cell-based reporter models for bone- and muscle-derived cell lines versus prostate-derived models
- Oral bioavailability in published rodent pharmacokinetic studies
Product Specifications
- Purity: ≥98% by HPLC, verified by third-party analytical testing
- Identity confirmation: HPLC; CHN elemental analysis on selected lots
Each batch is supplied with batch-specific Certificates of Analysis from independent third-party laboratories.
Research Applications
LGD-2226 is commonly referenced in laboratory research involving:
- Androgen receptor binding and competition assays
- SARM structure-activity relationship (SAR) analysis, particularly within the 2-quinolinone structural class
- Nuclear receptor selectivity profiling across the steroid hormone receptor family
- Analytical and reference-standard work, including mass spectrometric method development referenced in anti-doping analytical literature
- In vitro receptor pharmacology and ligand-binding domain conformation studies
- Comparative SARM evaluation alongside other nonsteroidal androgen receptor ligands
Storage & Handling
- Store powder at -20 °C for long-term stability
- Short-term storage at room temperature acceptable for active research use
- Protect from direct light
- Use desiccant for powder storage
- Close container tightly after each use
- Use appropriate laboratory handling procedures and PPE
Research Background & Regulatory Context
LGD-2226 is included on the World Anti-Doping Agency (WADA) Prohibited List under the anabolic agents category. This regulatory status is part of the published scientific and analytical record on the compound and reinforces that LGD-2226 is supplied strictly as a research reagent for laboratory and analytical use.
Research Use Disclaimer
LGD-2226 is intended strictly for laboratory research use only (RUO). Not for human consumption, clinical use, veterinary use, therapeutic application, or diagnostic use. All handling and use must comply with applicable federal, state, and local laws and institutional laboratory safety standards. This product is supplied exclusively to qualified researchers and scientific institutions.
| CAS Number | 328947-93-9 |
| Other Names | LGD-2226, LGD2226, LGD 2226 |
| IUPAC Name | 6-(bis-(2,2,2-trifluoromethyl)amino)-4-trifluoromethyl-1H-quinolin-2-one |
| Molecular Formula | C₁₄H₉F₉N₂O |
| Molecular Weight | 392.225 |
| Liquid Concentration And Solution | 10mg/ml PEG400, DMSO |
