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  3. BMS-687453

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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
Solid
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10 mg USD 180 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

444.86

Formula

C22H21ClN2O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (224.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.62 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
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]

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2479 mL 11.2395 mL 22.4790 mL 56.1975 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 mL 11.2395 mL
10 mM 0.2248 mL 1.1239 mL 2.2479 mL 5.6197 mL
15 mM 0.1499 mL 0.7493 mL 1.4986 mL 3.7465 mL
20 mM 0.1124 mL 0.5620 mL 1.1239 mL 2.8099 mL
25 mM 0.0899 mL 0.4496 mL 0.8992 mL 2.2479 mL
30 mM 0.0749 mL 0.3746 mL 0.7493 mL 1.8732 mL
40 mM 0.0562 mL 0.2810 mL 0.5620 mL 1.4049 mL
50 mM 0.0450 mL 0.2248 mL 0.4496 mL 1.1239 mL
60 mM 0.0375 mL 0.1873 mL 0.3746 mL 0.9366 mL
80 mM 0.0281 mL 0.1405 mL 0.2810 mL 0.7025 mL
100 mM 0.0225 mL 0.1124 mL 0.2248 mL 0.5620 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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