BMS 687453 |
Catalog No.GC15995 |
PPARα agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1000998-59-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Li J, et al. 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. |
IC50: 10 nM for human PPARα
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].
Clinical trial: Up to now, BMS 687453 is still in the preclinical development stage.
Reference:
[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.
Cas No. | 1000998-59-3 | SDF | |
Chemical Name | N-[[3-[[2-(4-chlorophenyl)-5-methyl-4-oxazolyl]methoxy]phenyl]methyl]-N-(methoxycarbonyl)-glycine | ||
Canonical SMILES | OC(CN(C(OC)=O)CC1=CC(OCC2=C(C)OC(C3=CC=C(Cl)C=C3)=N2)=CC=C1)=O | ||
Formula | C22H21ClN2O6 | M.Wt | 444.9 |
Solubility | DMSO: 30 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.2477 mL | 11.2385 mL | 22.477 mL |
5 mM | 0.4495 mL | 2.2477 mL | 4.4954 mL |
10 mM | 0.2248 mL | 1.1238 mL | 2.2477 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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