1. Cell Cycle/DNA Damage
  2. PPAR

BMS-687453 

Cat. No.: HY-10678 Purity: 99.70%
Handling Instructions

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.

For research use only. We do not sell to patients.

BMS-687453 Chemical Structure

BMS-687453 Chemical Structure

CAS No. : 1000998-59-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 145 In-stock
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Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
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Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
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Estimated Time of Arrival: December 31
25 mg USD 432 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
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Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
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Estimated Time of Arrival: December 31
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Customer Review

View All PPAR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target[1]

PPARα

260 nM (IC50, Human PPARα)

In Vitro

BMS-687453 is a potent and selective 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, 50, 100, p.o.) dose-dependently increases serum ApoA1 protein levels and low-density lipoprotein-cholesterol (LDLc) levels in mice. BMS-687453 (1, 3, 10 mg/kg, p.o.) decreases HDLc levels in high fat-fed hamsters[1]. BMS-687453 induces PDK4 mRNA in the liver, with ED50 value of 0.24 mg/kg[2]. BMS-687453 (300 mg/kg, p.o.) causes skeletal myofiber degeneration and necrosis characterized by observed discoid changes, myofibril lysis, hyalinization, and cellular infiltration in male rats. BMS-687453 (300 mg/kg, p.o.) induces a mild toxicity in both fast and slow-twitch muscles in male rats[3].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.2479 mL 11.2395 mL 22.4790 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 mL
10 mM 0.2248 mL 1.1239 mL 2.2479 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

A homogeneous, fluorescent polarization PPARα and PPARγ binding assay is used as the primary screen for determining the PPARα and PPARγ binding affinity of compounds. The human functional activity of PPARα and PPARγ agonists is determined by using the GAL4-LBD assays. The in vitro hamster, rat, and mouse PPARα functional activities are tested in the chimeric GAL4/PPARα assay format. The data are reported as an EC50 value calculated using XLfit 4 parameter fit and floating all parameters. Full length human PPARα and PPARγ co-transfection assays in HepG2 cells are employed for further testing the leading compounds (BMS-687453)[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

BMS-687453 is formulated in 2% Tween 80 and 0.5% CMC (carboxymethylcellulose) in 97.5% Gibco distilled water.

Male 6−8 week old human apoA1 transgenic mice are randomly assigned into different treatment groups and weighed and dosed by oral gavage (5 mL/kg body weight) once a day in the morning with vehicle alone or with compound (BMS-687453) and allowed free access to food and water. The study duration is 10 days. After dosing on day 10, mice are fasted for 4 h and sacrificed by CO2 asphyxiation, and blood samples are collected in serum-separating tubes via cardiac puncture for lipid measurements. Livers are dissected out, weighed, and quickly frozen in liquid nitrogen for future RNA analysis. Human apoA1 concentration in serum is measured using the apolipoprotein A1 kit[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

444.86

Formula

C₂₂H₂₁ClN₂O₆

CAS No.

1000998-59-3

SMILES

ClC(C=C1)=CC=C1C2=NC(COC3=CC=CC(CN(C(OC)=O)CC(O)=O)=C3)=C(C)O2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 31 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BMS-687453
Cat. No.:
HY-10678
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