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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $51 | In Stock | |
2 mg | $74 | In Stock | |
5 mg | $122 | In Stock | |
10 mg | $189 | In Stock | |
25 mg | $372 | In Stock | |
50 mg | $569 | In Stock | |
100 mg | $819 | In Stock | |
1 mL x 10 mM (in DMSO) | $173 | In Stock |
Description | Evacetrapib (LY2484595) (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3. |
In vitro | Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. Evacetrapib (LY2484595) (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells. [1] |
In vivo | Evacetrapib (LY2484595) (30 mg/kg, orally) results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4 hours, 8 hours and 24 hours post dose respectively in human ApoAI and CETP double transgenic mice. Evacetrapib (LY2484595) (30 mg/kg) results in 129.7% increase in HDL-C 8 hours after oral administration. The ED50 values of CETP inhibitory activity 8 hours post oral dosing for Evacetrapib (LY2484595) in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. Evacetrapib (LY2484595) (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats. [1] |
Kinase Assay | Human CETP cDNA is amplified from a human liver cDNA library and the sequence is confirmed to be identical to the published sequence. The cDNA is subcloned into a pcDNA3.1 vector, under the control of CMV promoter. A stable line is established in CV1 cells in which the above-mentioned construct is used to express the recombinant human CETP. The medium contained the secreted recombinant CETP protein and the amount (19 ng/μL) is quantified by an ELISA kit. The medium is then aliquoted in 0.2% BSA and stored at -80°C. The stock CETP protein is diluted 150-fold in CETP buffer (10 mM Tris, 150 mM NaCl, and 2 mM EDTA) before use. The assay is set up in a 96-well plate. Each well received 97.5 μL diluted CETP protein (final concentration 7 nM) and 2.5 μL of compound stock. After a 30 min incubation at 37°C, 5 μL of substrate stock (the same stock used in the human plasma CETP assay), 0.16 μL of VLDL stock (2.5 mg/mL, Intracel) and 145 μL of CETP buffer are added, and the incubation is continued for another 4 h. Signal is read for the human plasma CETP assay[1]. |
Alias | LY2484595 |
Molecular Weight | 638.65 |
Formula | C31H36F6N6O2 |
Cas No. | 1186486-62-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 13 mg/mL (20.4 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 11 mg/mL (17.2 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
DMSO
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