化合物 BMS-687453|T5532|TargetMol

BMS-687453
1000998-59-3

￥197 1mg 起订

￥491 5mg 起订

￥768 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 BMS-687453

英文名称：: BMS-687453

CAS号：: 1000998-59-3

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.40%

产品类别：: 抑制剂

货号：: T5532

Product Introduction

Bioactivity

名称	BMS-687453
描述	BMS-687453 is a potent and selective PPAR alpha agonist, with an EC(50) of 10 nM for human PPARalpha and approximately 410-fold selectivity vs human PPARgamma in PPAR-GAL4 transactivation assays.
激酶实验	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].
动物实验	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].
体外活性	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].
体内活性	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]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 31 mg/mL (69.68 mM)
关键字	PPAR \| BMS687453 \| Peroxisome proliferator-activated receptors \| BMS-687453 \| BMS 687453 \| Inhibitor \| inhibit
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BMS-687453|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务