1000998-59-3 Usage
Biological Activity
bms 687453 is a pparα agonist.the peroxisome proliferator activated receptor (ppar) is a member of the intracellular nuclear hormone receptor superfamily of transcription factors, having pleiotropic effects on plasma lipoprotein levels, insulin sensitization, atherosclerosis, and inflammation.
in vitro
bms-687453 was identified as a potent and selective ppar alpha agonist, with approximately 410-fold selectivity versus human ppargamma in ppar-gal4 transactivation assays. in addition, similar potency and selectivity were also seen in the full length receptor co-transfection assays. [1].
in vivo
in previous study, bms-687453 had an excellent pharmacokinetic profile across all tested animal species. the oral absorption was rapid in mouse, rat, dog, and cynomulgus monkey. bms-687453 also exhibited low plasma clearance in the mouse, rat, and monkey and moderate plasma clearance in the dog. the half-life of bms-687453 ranged from 3 h in mouse to 12 h in cynomolgus monkeys. bms-687453 showed excellent absolute oral bioavailability ranging from 58% (dog) to 91% (rat) [1].
IC 50
10 nm for human pparα
references
[1] li j. discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl) amino)acetic acid (bms-687453). j med chem. 2010 apr 8;53(7):2854-64.
Check Digit Verification of cas no
The CAS Registry Mumber 1000998-59-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,0,0,9,9 and 8 respectively; the second part has 2 digits, 5 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1000998-59:
(9*1)+(8*0)+(7*0)+(6*0)+(5*9)+(4*9)+(3*8)+(2*5)+(1*9)=133
133 % 10 = 3
So 1000998-59-3 is a valid CAS Registry Number.
1000998-59-3Relevant articles and documents
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor α selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4- yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453)
Li, Jun,Kennedy, Lawrence J.,Shi, Yan,Tao, Shiwei,Ye, Xiang-Yang,Chen, Stephanie Y.,Wang, Ying,Hernández, Andrés S.,Wang, Wei,Devasthale, Pratik V.,Chen, Sean,Lai, Zhi,Zhang, Hao,Wu, Shung,Smirk, Rebecca A.,Bolton, Scott A.,Ryono, Denis E.,Zhang, Huiping,Lim, Ngiap-Kie,Chen, Bang-Chi,Locke, Kenneth T.,O'Malley, Kevin M.,Zhang, Litao,Srivastava, Rai Ajit,Miao, Bowman,Meyers, Daniel S.,Monshizadegan, Hossain,Search, Debra,Grimm, Denise,Zhang, Rongan,Harrity, Thomas,Kunselman, Lori K.,Cap, Michael,Kadiyala, Pathanjali,Hosagrahara, Vinayak,Zhang, Lisa,Xu, Carrie,Li, Yi-Xin,Muckelbauer, Jodi K.,Chang, Chiehying,An, Yongmi,Krystek, Stanley R.,Blanar, Michael A.,Zahler, Robert,Mukherjee, Ranjan,Cheng, Peter T. W.,Tino, Joseph A.
experimental part, p. 2854 - 2864 (2010/08/22)
An 1,3-oxybenzylglycine based compound 2 (BMS-687453) was discovered to be a potent and selective peroxisome proliferator activated receptor (PPAR) α agonist, with an EC50 of 10 nM for human PPARα and -410-fold selectivity vs human PPAR- in PPA
