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BMS-687453

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Catalog No. T5532Cas No. 1000998-59-3

BMS-687453 is a potent and selective PPAR alpha agonist, demonstrating an EC(50) of 10 nM for human PPAR alpha and approximately 410-fold selectivity versus human PPAR gamma in PPAR-GAL4 transactivation assays.

BMS-687453

BMS-687453

🥰Excellent
Purity: 99.40%
Catalog No. T5532Cas No. 1000998-59-3
BMS-687453 is a potent and selective PPAR alpha agonist, demonstrating an EC(50) of 10 nM for human PPAR alpha and approximately 410-fold selectivity versus human PPAR gamma in PPAR-GAL4 transactivation assays.
Pack SizePriceAvailabilityQuantity
1 mg37 €In Stock
2 mg52 €In Stock
5 mg84 €In Stock
10 mg139 €In Stock
25 mg282 €In Stock
50 mg432 €In Stock
100 mg654 €In Stock
1 mL x 10 mM (in DMSO)93 €In Stock
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Purity:99.40%
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Product Introduction

Bioactivity
Description
BMS-687453 is a potent and selective PPAR alpha agonist, demonstrating an EC(50) of 10 nM for human PPAR alpha and approximately 410-fold selectivity versus human PPAR gamma in PPAR-GAL4 transactivation assays.
Targets&IC50
PPARα (human):260 nM
In vitro
BMS-687453 is PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and ~410-fold and more than 57-fold selectivity vs human PPARγ of 4100 nM and >15000 nM in PPAR-GAL4 transactivation assays. BMS-687453 exhibits high PPARα potency (EC50: 47 nM) with ~50-fold selectivity vs PPARγ (EC50: 2400 nM) in HepG2 cells. However, BMS-687453 shows less potent activities in rodent PPARα functional assays, with a moderate EC50 of 426 nM for mouse and 488 nM for hamster but remains a full PPARα agonist in both species [1].
In vivo
BMS 687453 (10-100 mg/kg) reduces plasma triglyceride levels and increases HDL levels in human ApoA1 transgenic mice. It also reduces serum triglyceride and LDL levels in hamsters fed a high-fat diet[2]
Kinase Assay
A homogeneous, fluorescent polarization PPARR and PPARγ binding assay was used as the primary screen for determining the PPARR and PPARγ binding affinity of compounds. The human functional activity of PPARR and PPARγ agonists was determined by using the GAL4-LBD assays as previously described. The in vitro hamster, rat, and mouse PPARR functional activities were tested in the chimeric GAL4/PPARR assay format described for human PPARR as above. The data are reported as an EC50 value calculated using XLfit 4 parameter fit and floating all parameters. Full-length human PPARR and PPARγ co-transfection assays in HepG2 cells were employed for further testing the leading compounds (BMS-687453) [1].
Animal Research
Male Syrian golden hamsters were acclimated to 12 h light/dark reverse light cycle for 7 days with high fat diet, then dosed daily by oral gavage for 21 days while on the same diet. At the end of the experiment, blood samples were drawn retro-orbitally after an 18 h fast and 24 h after the last dose for the determination of serum lipid levels. Livers were dissected out for mRNA analysis [1].
Chemical Properties
Molecular Weight444.86
FormulaC22H21ClN2O6
Cas No.1000998-59-3
SmilesCOC(=O)N(CC(O)=O)Cc1cccc(OCc2nc(oc2C)-c2ccc(Cl)cc2)c1
Relative Density.1.342 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 31 mg/mL (69.68 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2479 mL11.2395 mL22.4790 mL112.3949 mL
5 mM0.4496 mL2.2479 mL4.4958 mL22.4790 mL
10 mM0.2248 mL1.1239 mL2.2479 mL11.2395 mL
20 mM0.1124 mL0.5620 mL1.1239 mL5.6197 mL
50 mM0.0450 mL0.2248 mL0.4496 mL2.2479 mL

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