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Evacetrapib

Cat. No. M2330

Evacetrapib Structure

Synonym: LY2484595

Size Price Availability Quantity
10mg USD 220 In stock
50mg USD 750 In stock
100mg USD 1250 In stock
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Biological Activity

Evacetrapib (investigational name LY2484595) is a potent and selective inhibitor of CETP both in vitro and in vivo. Evacetrapib inhibits cholesterylester transfer protein, which transfers and thereby increases high-density lipoprotein and lowers low-density lipoprotein. In double transgenic mice expressing human CETP and apoAI, evacetrapib exhibited an ex vivo CETP inhibition ED(50) of less than 5 mg/kg at 8 h post oral dose and significantly elevated HDL cholesterol. In addition, in a human adrenal cortical carcinoma cell line (H295R cells), evacetrapib did not induce aldosterone or cortisol biosynthesis whereas torcetrapib dramatically induced aldosterone and cortisol biosynthesis.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 638.65
Formula C31H36F6N6O2
CAS Number 1186486-62-3
Purity 98.86%
Solubility DMSO
Storage at -20°C
References

Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure.
Cao G, et al. J Lipid Res. 2011 Dec;52(12):2169-76. PMID: 21957197.

Related CETP Products
Dalcetrapib

Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol.

Anacetrapib

Anacetrapib is an orally active and potent inhibitor of CETP with IC50 of 7.9 nM and 11.8 nM for rhCETP and mutant CETP(C13S) respectively.

Torcetrapib

Torcetrapib (CP-529414) is a prototype cholesteryl ester transfer protein (CETP) inhibitor with potential for decreasing atherosclerotic disease, increased cardiovascular events in clinical trials.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Evacetrapib, LY2484595 supplier, CETP, inhibitors

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