BMS-687453 NEW
| Price | $39 | $55 | $89 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: BMS-687453 | CAS No.: 1000998-59-3 |
| Purity: 99.40% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | BMS-687453 |
| 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. |
| 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]. |
| 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] |
| Storage | Powder: -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) |
| Keywords | PPAR | BMS687453 | Peroxisome proliferator-activated receptors | BMS-687453 | BMS 687453 | Inhibitor | inhibit |
| Inhibitors Related | PHYTOL | (S)-(+)-Ibuprofen | BADGE | Cinnamyl alcohol | Daidzein | Fenofibrate | Pioglitazone hydrochloride | 5-Aminosalicylic Acid | Naringenin | Fisetin | 2,3-Butanediol | Icariin |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Anti-Breast Cancer Compound Library | Anti-Obesity Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Hypertension Compound Library | Transcription Factor-Targeted Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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