BMS-687453 Chemical Properties

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

BMS-687453 Usage And Synthesis

Uses

BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.

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.