Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-687453 是一种选择性 PPARα激动剂,对人 PPARα的 EC50和 IC50分别为 10 nM 和 260 nM。它较弱地抑制 PPARγ 的活性,EC50和 IC50值分别为 4100 nM 和大于 15000 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
2 mg | ¥ 483 | 现货 | ||
5 mg | ¥ 818 | 现货 | ||
10 mg | ¥ 1,280 | 现货 | ||
25 mg | ¥ 2,590 | 现货 | ||
50 mg | ¥ 3,960 | 现货 | ||
100 mg | ¥ 6,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 981 | 现货 |
产品描述 | 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. |
靶点活性 | PPARα (human):260 nM |
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] |
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]. |
分子量 | 444.86 |
分子式 | C22H21ClN2O6 |
CAS No. | 1000998-59-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31 mg/mL (69.68 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2479 mL | 11.2395 mL | 22.479 mL | 56.1975 mL |
5 mM | 0.4496 mL | 2.2479 mL | 4.4958 mL | 11.2395 mL | |
10 mM | 0.2248 mL | 1.1239 mL | 2.2479 mL | 5.6197 mL | |
20 mM | 0.1124 mL | 0.562 mL | 1.1239 mL | 2.8099 mL | |
50 mM | 0.045 mL | 0.2248 mL | 0.4496 mL | 1.1239 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BMS-687453 1000998-59-3 DNA Damage/DNA Repair Metabolism PPAR BMS687453 Peroxisome proliferator-activated receptors BMS 687453 Inhibitor inhibit inhibitor