BMS 687453

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BMS 687453

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1000998-59-3

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价

化学性质

Storage	Store at -20°C
M.Wt	444.9
Cas No.	1000998-59-3
Formula	C₂₂H₂₁ClN₂O₆
Solubility	Soluble in DMSO
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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.