Bioactivity | GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia[1]. |
In Vivo | GW 590735 (0.5-5 mg/kg; orally twice a day for 5 days) is able to lower LDLc and triglycerides (TG) and increase HDL cholesterol in the Apo-A-I-transgenic mouse model (male C57BL/6 mice transgenic for human ApoA-I)[1].GW 590735 (intravenous administration; 2.7 mg/kg; rat) treatment shows Cl, Vd, T1/2, and F% are 5 mL/min/kg, 1 L/kg, 2.4 hours and 47%, respectively[1].GW 590735 (intravenous administration; 2 mg/kg; dog) treatment shows Cl, Vd, T1/2, and F% are 13 mL/min/kg, 2.8 L/kg, 2.6 hours and 85%, respectively[1]. |
Name | GW 590735 |
CAS | 343321-96-0 |
Formula | C23H21F3N2O4S |
Molar Mass | 478.48 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
Reference | [1]. Sierra ML, et al. Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents. J Med Chem. 2007;50(4):685-695. |