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BMS-687453
CAS No. 1000998-59-3
BMS-687453( BMS687453 | BMS 687453 )
Catalog No. M10011 CAS No. 1000998-59-3
A potent and selective PPARα agonist with EC50 of 10 nM for human PPARα and 410-fold selectivity over human PPARγ in PPAR-GAL4 transactivation assays.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 58 | In Stock |
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| 5MG | 88 | In Stock |
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| 10MG | 162 | In Stock |
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| 25MG | 332 | In Stock |
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| 50MG | 494 | In Stock |
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| 100MG | 709 | In Stock |
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| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameBMS-687453
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NoteResearch use only, not for human use.
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Brief DescriptionA potent and selective PPARα agonist with EC50 of 10 nM for human PPARα and 410-fold selectivity over human PPARγ in PPAR-GAL4 transactivation assays.
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DescriptionA potent and selective PPARα agonist with EC50 of 10 nM for human PPARα and 410-fold selectivity over human PPARγ in PPAR-GAL4 transactivation assays; has negligible cross-reactivity against a panel of human nuclear hormone receptors including PPARδ; demonstrates an excellent pharmacological and safety profile for the treatment of atherosclerosis and dyslipidemia.Dyslipidemia Preclinical
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In VitroBMS-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.
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In VivoBMS-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. BMS-687453 induces PDK4 mRNA in the liver, with ED50 value of 0.24 mg/kg. 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.
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SynonymsBMS687453 | BMS 687453
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PathwayMetabolic Enzyme/Protease
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TargetPPAR
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RecptorPPAR
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Research AreaCardiovascular Disease
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IndicationDyslipidemia
Chemical Information
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CAS Number1000998-59-3
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Formula Weight444.8649
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Molecular FormulaC22H21ClN2O6
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 31 mg/mL
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SMILESO=C(O)CN(CC1=CC=CC(OCC2=C(C)OC(C3=CC=C(Cl)C=C3)=N2)=C1)C(OC)=O
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Chemical NameGlycine, N-[[3-[[2-(4-chlorophenyl)-5-methyl-4-oxazolyl]methoxy]phenyl]methyl]-N-(methoxycarbonyl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Li J, et al. J Med Chem. 2010 Apr 8;53(7):2854-64.
2. Mukherjee R, et al. J Pharmacol Exp Ther. 2008 Dec;327(3):716-26.
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