211513-37-0 Usage
Uses
Different sources of media describe the Uses of 211513-37-0 differently. You can refer to the following data:
1. Dalcetrapib is a cholesteryl ester transfer protein (CETP) inhibitor. Dalcetrapib is a drug undergoing trials for the treatment of cardiovascular disease, dyslipidemia, peripheral arterial disease (PA
D).
2. Dalcetrapib is a cholesteryl ester transfer protein (CETP) inhibitor. Dalcetrapib is a drug undergoing trials for the treatment of cardiovascular disease, dyslipidemia, peripheral arterial disease (PAD).
Biological Activity
cholesteryl ester transfer protein (cetp) is a plasma protein that transfers neutral lipids among the lipoproteins. its most important action is the exchange of cholesteryl esters in high-density lipoprotein (hdl) for triglycerides in very low-density lipoprotein. thus, cetp is a potentially atherogenic protein, and its atherogenicity has been supported by many studies. dalcetrapib is a novel inhibitors of cetp.
in vitro
dalcetrapib achieved 50% inhibition of cetp activity in human plasma at a concentration of 6 μm. the mechanism of action was considered to involve the formation of a disulfide bond between the thiol form of dalcetrapib and the cysteine residue at position 13 (cys13) of cetp. [1].
in vivo
dalcetrapib achieved 95% inhibition of cetp activity in male japanese white rabbits at an oral dose of 30 mg/kg. it increased the plasma hdl cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 or 100 mg/kg once a day for 3 days to male japanese white rabbits [1].
IC 50
6 μm for cetp inhibition in human plasma
references
[1] 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;43(19):3566-72.[2] fayad za, mani v, woodward m, kallend d, abt m, burgess t, fuster v, ballantyne cm, stein ea, tardif jc, rudd jh, farkouh me, tawakol a. safety and efficacy of dalcetrapib on atherosclerotic disease using novel non-invasive multimodality imaging (dal-plaque): a randomised
Check Digit Verification of cas no
The CAS Registry Mumber 211513-37-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,1,1,5,1 and 3 respectively; the second part has 2 digits, 3 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 211513-37:
(8*2)+(7*1)+(6*1)+(5*5)+(4*1)+(3*3)+(2*3)+(1*7)=80
80 % 10 = 0
So 211513-37-0 is a valid CAS Registry Number.
211513-37-0Relevant articles and documents
New Process
-
Page/Page column 14, (2012/06/30)
The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is useful as a pharmaceutically active compound.
NOVEL PROCESS
-
Page/Page column 9, (2011/01/12)
The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is a useful pharmaceutical active compound.
CETP activity inhibitors
-
, (2008/06/13)
The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof. The compounds represented by the formula (I) can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity and, therefore, is expected to be useful as a new type of a preventive or therapeutic agent for atherosclerosis or hyperlipidemia.