Molecular Formula | C31H36F6N6O2 |
Molar Mass | 638.65 |
Density | 1.40 |
Boling Point | 680.1±65.0 °C(Predicted) |
pKa | 4.73±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | Evacetrapib (LY2484595) inhibits human plasma CETP protein with an IC50 of 26 nM. There was no induction of aldosterone or cortisol synthesis by the action of Evacetrapib (LY2484595)(< 10 μm) on H295R cells. Evacetrapib (LY2484595) inhibits human plasma CETP protein with an IC50 of 26 nM. There was no induction of aldosterone or cortisol synthesis by the action of Evacetrapib (LY2484595)(< 10 μm) on H295R cells. |
In vivo study | Human ApoAI and CETP double transgenic mice were orally treated with a dose of 30 mg/kg of Evacetrapib (LY2484595) and inhibited by 98.4%, 98.6%, respectively after 4 hours, 8 hours and 12 hours of treatment, and 18.4% CETP activity. After 8 hours of oral treatment with Evacetrapib (LY2484595)(30 mg/kg) resulted in an increase of 129.7% HDL-C. In a dose-response study, the ED50 values for inhibition of CETP activity were 3.5 mg/kg and 4.1 mg/kg, respectively, after 8 hours of oral treatment with Evacetrapib(LY2484595). Evacetrapib(LY2484595)(< 200 mg/kg) treatment of Zucker diabetic obese rats did not increase blood pressure. human ApoAI and CETP double transgenic mice were orally treated with a dose of 30 mg/kg of Evacetrapib (LY2484595) and inhibited by 98.4% after 4 hours, 8 hours, and 12 hours of treatment, respectively, 98.6%, and 18.4% CETP activity. After 8 hours of oral treatment with Evacetrapib (LY2484595)(30 mg/kg) resulted in an increase of 129.7% HDL-C. In a dose-response study, the ED50 values for inhibition of CETP activity were 3.5 mg/kg and 4.1 mg/kg, respectively, after 8 hours of oral treatment with Evacetrapib(LY2484595). Evacetrapib(LY2484595)(< 200 mg/kg) treatment of Zucker diabetic obese rats did not increase blood pressure. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.566 ml | 7.829 ml | 15.658 ml |
5 mM | 0.313 ml | 1.566 ml | 3.132 ml |
10 mM | 0.157 ml | 0.783 ml | 1.566 ml |
5 mM | 0.031 ml | 0.157 ml | 0.313 ml |