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- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
BMS-687453
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1000998-59-3
- 规格：
5mg/10mg/25mg/1mg/50mg
| 规格： | 5mg | 产品价格： | ¥980.00 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ¥1570.00 |
| 规格： | 25mg | 产品价格： | ¥3140.00 |
| 规格： | 1mg | 产品价格： | ¥390.00 |
| 规格： | 50mg | 产品价格： | ¥4870.00 |
| CAS | 1000998-59-3 |
| 英文名称 | BMS-687453 |
| 别名 | ;UNII-39TL5L7XDX;7HA;dimethyldiadzein; |
| 分子式 | C22H21ClN2O6 |
| 分子量 | 444.9 |
| 规格 | 10mg ; 25mg ; 5mg ; 1mg ; 50mg |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷冻运输 |
| MDL | MFCD18251482 |
| SMILES | CC1=C(N=C(O1)C2=CC=C(C=C2)Cl)COC3=CC=CC(=C3)CN(CC(=O)O)C(=O)OC |
| InChIKey | UJIBXDMNCMEJAY-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H21ClN2O6/c1-14-19(24-21(31-14)16-6-8-17(23)9-7-16)13-30-18-5-3-4-15(10-18)11-25(12-20(26)27)22(28)29-2/h3-10H，11-13H2，1-2H3，(H，26，27) |
| PubChem CID | 16725047 |
| 靶点 | PPAR |
| 通路 | Cell Cycle;DNA Damage/DNA Repair;Metabolic Enzyme&Protease |
| 背景说明 | BMS-687453是一种有效的,选择性的 PPARα 激动剂。 |
| 生物活性 | BMS-687453 is a potent and selective PPARα agonist， with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.[1-3] |
| In Vitro | BMS-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[1]. |
| In Vivo | BMS-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[1]. BMS-687453 induces PDK4 mRNA in the liver，with ED50 value of 0.24 mg/kg[2]. 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[3]. |
| 动物实验 | 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]. |
| 激酶实验 | 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]. |
| 数据来源文献 | [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 [2]. Mukherjee R， et al. Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides， raise high-density lipoprotein， and synergistically increase cholesterol excretion with a liver X receptor agonist. J Phar [3]. Vassallo JD， et al. Biomarkers of drug-induced skeletal muscle injury in the rat: troponin I and myoglobin. Toxicol Sci. 2009 Oct;111(2):402-12. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|2.2477mL|11.2385mL|22.477mL|$$|5mM|0.4495mL|2.2477mL|4.4954mL|$$|10mM|0.2248mL|1.1238mL|2.2477mL| |
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