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Chemical Structure| 1186486-62-3 Chemical Structure| 1186486-62-3

Structure of Evacetrapib
CAS No.: 1186486-62-3

Chemical Structure| 1186486-62-3

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Evacetrapib is a potent and selective inhibitor of CETP with IC50 of 5.5 nM.

Synonyms: LY2484595

4.5 *For Research Use Only !

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Product Details of Evacetrapib

CAS No. :1186486-62-3
Formula : C31H36F6N6O2
M.W : 638.65
SMILES Code : O=C([C@H]1CC[C@H](CN2C3=C(C)C=C(C)C=C3[C@@H](N(CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C5=NN(C)N=N5)CCC2)CC1)O
Synonyms :
LY2484595
MDL No. :MFCD23105886
InChI Key :IHIUGIVXARLYHP-UXNJHFGPSA-N
Pubchem ID :49836058

Safety of Evacetrapib

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H228-H315-H319
Precautionary Statements:P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
Class:4.1
UN#:1325
Packing Group:

Isoform Comparison

Biological Activity

Target
  • CETP

    CETP, IC50:5.5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse primary hepatocytes 1–10 µM 24 hours Evacetrapib similarly inhibits LDLR and PCSK9 expression in CETP-negative cells PMC4539152
HepG2 cells 1–10 µM 24 hours Evacetrapib inhibits LDLR and PCSK9 expression by reducing the mature form of SREBP2 PMC4539152
Human recombinant cytochromes P450 (rCYPs) 30 or 300 nM 5 or 30 minutes To evaluate the metabolic pathways of Evacetrapib and the contribution of CYP enzymes. Results showed that CYP3A was responsible for about 90% of CYP-associated clearance, while CYP2C8 accounted for about 10%. PMC4618649

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Human CETP and ApoAI double transgenic mice Oral 30 mg/kg Single dose To evaluate the inhibition of CETP activity and the effect on HDL cholesterol levels by Evacetrapib, results showed significant inhibition of CETP activity and elevation of HDL cholesterol levels PMC3220285
Transgenic mice CETP transgenic mice Tail vein injection 40 mg/kg and 120 mg/kg Single injection, observed for 24 hours To evaluate the pharmacokinetic parameters of Evacetrapib in plasma, liver, and brain tissues, results showed that Evacetrapib can cross the blood-brain barrier and was detected in brain tissue PMC10390775

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01825889 Cardiovascular Disease PHASE1 COMPLETED 2025-10-13 For additional information reg... More >>arding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Miami, Florida, 33014, United States|For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Orlando, Florida, 32806, United States|For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Saint Paul, Minnesota, 55114, United States Less <<
NCT02226653 Healthy Volunteers PHASE1 COMPLETED 2025-04-15 For additional information reg... More >>arding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Fukuoka, 812-0025, Japan Less <<
NCT02497391 Healthy PHASE1 COMPLETED 2025-11-15 For additional information reg... More >>arding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Singapore, 117597, Singapore Less <<
NCT01903434 Healthy Volunteers PHASE1 COMPLETED 2025-11-13 For additional information reg... More >>arding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Evansville, Indiana, 47710, United States Less <<
NCT02168803 Dyslipidemia PHASE1 COMPLETED 2025-12-15 Covance Clinical Research Inc,... More >> Daytona Beach, Florida, 32117, United States|Covance, Dallas, Texas, 75247, United States|Covance Clinical Research Inc, Madison, Wisconsin, 53704, United States Less <<
NCT01836185 Hepatic Insufficiency PHASE1 COMPLETED 2025-10-13 For additional information reg... More >>arding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Miami, Florida, 33169, United States|For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Orlando, Florida, 32806, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.83mL

1.57mL

0.78mL

15.66mL

3.13mL

1.57mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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