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Evacetrapib

Catalog No. T6262 CAS 1186486-62-3

Synonyms: LY2484595

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.

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Evacetrapib, CAS 1186486-62-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
2 mg	In stock	$ 74.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 189.00
25 mg	In stock	$ 372.00
50 mg	In stock	$ 569.00
100 mg	In stock	$ 819.00
1 mL * 10 mM (in DMSO)	In stock	$ 173.00

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Purity: 98.53%

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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.
Targets&IC50	CETP:5.5 nM
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].

Synonyms	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)

References and Literature

1. Cao G, et al. J Lipid Res, 2011, 52(12), 2169-2176.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Anti-Obesity Compound Library Clinical Compound Library NO PAINS Compound Library Human Metabolite Library Bioactive Compound Library ReFRAME Related Library Anti-Cardiovascular Disease Compound Library Bioactive Compounds Library Max

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Keywords

Evacetrapib 1186486-62-3 Metabolism CETP inhibit LY-2484595 Inhibitor LY 2484595 LY2484595 Cholesteryl ester transfer protein inhibitor

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