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Chemical Structure| 211513-37-0 Chemical Structure| 211513-37-0

Structure of Dalcetrapib
CAS No.: 211513-37-0

Chemical Structure| 211513-37-0

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Dalcetrapib is a rhCETP inhibitor with IC50 of 0.2 μM.

Synonyms: RO4607381; JTT-705

4.5 *For Research Use Only !

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Product Details of Dalcetrapib

CAS No. :211513-37-0
Formula : C23H35NO2S
M.W : 389.59
SMILES Code : CC(C)C(SC1=CC=CC=C1NC(C2(CC(CC)CC)CCCCC2)=O)=O
Synonyms :
RO4607381; JTT-705
MDL No. :MFCD06407886
InChI Key :YZQLWPMZQVHJED-UHFFFAOYSA-N
Pubchem ID :6918540

Safety of Dalcetrapib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Dalcetrapib

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • CETP

    rhCETP, IC50:0.2 μM

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.83mL

2.57mL

1.28mL

25.67mL

5.13mL

2.57mL

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

[1]Niesor EJ, Magg C, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010 Dec;51(12):3443-54.

[2]Shinkai H, Maeda K, et al. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem. 2000 Sep 21;43(19):3566-72.

[3]Takubo H, Ishikawa T, et al. Pharmacokinetics and disposition of dalcetrapib in rats and monkeys. Xenobiotica. 2014 Dec;44(12):1117-26.

[4]Briand F, Thieblemont Q, et al. Anacetrapib and dalcetrapib differentially alters HDL metabolism and macrophage-to-feces reverse cholesterol transport at similar levels of CETP inhibition in hamsters. Eur J Pharmacol. 2014 Oct 5;740:135-43.

[5]Shinkai H, Maeda K, et al. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem. 2000 Sep 21;43(19):3566-72.

[6]Kuhlmann O, Heinig K, et al. Dalcetrapib pharmacokinetics and metabolism in the cynomolgus monkey. Xenobiotica. 2011 May;41(5):430-6.

[7]Kosmas CE, DeJesus E, Rosario D, Vittorio TJ. CETP Inhibition: Past Failures and Future Hopes. Clin Med Insights Cardiol. 2016 Mar 13;10:37-42. doi: 10.4137/CMC.S32667. PMID: 26997876; PMCID: PMC4790583.

[8]Niesor EJ, Magg C, Ogawa N, Okamoto H, von der Mark E, Matile H, Schmid G, Clerc RG, Chaput E, Blum-Kaelin D, Huber W, Thoma R, Pflieger P, Kakutani M, Takahashi D, Dernick G, Maugeais C. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010 Dec;51(12):3443-54. doi: 10.1194/jlr.M008706. Epub 2010 Sep 22. PMID: 20861162; PMCID: PMC2975716.

[9]Shinkai H, Maeda K, Yamasaki T, Okamoto H, Uchida I. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem. 2000 Sep 21;43(19):3566-72. doi: 10.1021/jm000224s. PMID: 11000011.

[10]Huang Z, Inazu A, Kawashiri MA, Nohara A, Higashikata T, Mabuchi H. Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells. Am J Physiol Endocrinol Metab. 2003 Jun;284(6):E1210-9. doi: 10.1152/ajpendo.00453.2002. Epub 2003 Feb 25. PMID: 12604506.

 

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