| Identification | Back Directory | [Name]
BMS-687453 | [CAS]
1000998-59-3 | [Synonyms]
CS-1533
BMS-687453
BMS-687453;BMS687453;BMS 687453
N-(3-{[2-(4-Chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}benzyl)-N-(methoxycarbonyl)glycine
N-[[3-[[2-(4-Chlorophenyl)-5-methyl-4-oxazolyl]methoxy]phenyl]methyl]-N-(methoxycarbonyl)glycine
Glycine, N-[[3-[[2-(4-chlorophenyl)-5-methyl-4-oxazolyl]methoxy]phenyl]methyl]-N-(methoxycarbonyl)-
2-[[3-[[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy]phenyl]methyl-methoxycarbonylamino]acetic acid | [Molecular Formula]
C22H21ClN2O6 | [MDL Number]
MFCD18251482 | [MOL File]
1000998-59-3.mol | [Molecular Weight]
444.86 |
| Chemical Properties | Back Directory | [Boiling point ]
642.7±65.0 °C(Predicted) | [density ]
1.342±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
Soluble in DMSO | [form ]
A crystalline solid | [pka]
3.93±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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. |
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