LY2562175 is a potent and selective FXR agonist in vitro and has robust lipid modulating properties, lowering LDL and triglycerides while raising HDL in preclinical species. The preclinical ADME properties of LY2562175 were consistent with enabling once daily dosing in humans, and it was ultimately advanced to the clinic for evaluation in humans. LY2562175 promotes transcriptional activation of human FXR in a cell-based cotransfection assay with an EC50 of 193 nM (geometric mean).
MedKoo Cat#: 522514
Name: LY2562175
CAS#: 1103500-20-4 (free acid)
Chemical Formula: C28H27Cl2N3O4
Exact Mass: 539.1379
Molecular Weight: 540.44
Elemental Analysis: C, 62.23; H, 5.04; Cl, 13.12; N, 7.78; O, 11.84
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 20.0 | 37.01 | |
| DMSO | 64.2 | 118.73 | |
| DMSO:PBS (pH 7.2) (1:3) | 0.3 | 0.46 | |
| Ethanol | 1.5 | 2.78 |
The following data is based on the product molecular weight 540.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
