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Evacetrapib

Cat. No. M2330
Evacetrapib Structure
Synonym:

LY2484595

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 90  USD90 In stock
5mg USD 140  USD140 In stock
10mg USD 210  USD210 In stock
50mg USD 750  USD750 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 638.65
Formula C31H36F6N6O2
CAS Number 1186486-62-3
Solubility (25°C) DMSO 14 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Cao G, et al. J Lipid Res. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure.

Related CETP Products
Obicetrapib

Obicetrapib is a selective, orally active cholesterol transporter protein (CETP) inhibitor that blocks the function of CETP and significantly reduces LDL-C while significantly increasing HDL-C levels, and may be used in studies related to atherosclerosis and Alzheimer's disease (AD).

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.

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Keywords: Evacetrapib, LY2484595 supplier, CETP, inhibitors, activators


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