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- CAS号：
196808-24-9
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥668.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥279.0 |
| 规格： | 5mg | 产品价格： | ￥610.0 |
| 规格： | 10mg | 产品价格： | ￥1064.0 |
| 规格： | 25mg | 产品价格： | ￥2344.0 |
| 规格： | 50mg | 产品价格： | ￥3464.0 |
| 规格： | 100mg | 产品价格： | ￥4944.0 |
Product Introduction
Bioactivity
| 名称 | GW1929 |
| 描述 | GW1929 is a potent PPAR-γ agonist (pKi: 8.84 for human PPAR-γ; pEC50s of 8.56 and 8.27 for human and murine PPAR-γ). |
| 细胞实验 | For the experiments, the cells are plated in 96-well plates at a density of 2 × 10^5 cells per cm2 and cultured in the presence of TBBPA, in concentrations ranging from 1 nM to 100 μM TBBPA. TBBPA is dissolved in DMSO, resulting in a final vehicle concentration of 0.1 % (v/v). Control (no vehicle) and DMSO-treated wells are included in the experimental design to determine the effect of DMSO. To study whether PPAR-γ is involved in the neurotoxic effect of TBBPA, cells are co-treated with 10 μM TBBPA and 10 μM GW1929 or GW9662. After 6 or 24 h of culture, 100 μL medium is collected for the LDH analysis, and the cells are collected and frozen at ?70°C for the caspase-3 activity measurements [2]. |
| 激酶实验 | Ligand binding to bacterially expressed ligand-binding domain (LBD) of hPPAR-γ is determined by the scintillation proximity assay (SPA). The assay measures the ability of putative ligands to displace receptor-bound [3H]BRL 49653. Assays are conducted in 96-well plates. Wells contained varying concentrations of GW1929 or troglitazone; streptavidin-modified SPA beads to which biotinylated PPAR-γ LBD is prebound; and 10 nM of the specific radioligand [3H]BRL 49653 in a volume of 100 μL. The amount of nonspecific binding, as assessed by control wells that contained 50 μM of the corresponding unlabeled ligand, is subtracted from each data point. For each compound tested, plots of ligand concentration versus counts/min of radioligand bound are constructed, and apparent Ki values are estimated from a nonlinear least-squares fit of the data, assuming simple competitive binding. The results are expressed as pKi, where pKi = -log10(KI) [1]. |
| 动物实验 | Animals are housed at 72°F and 50% relative humidity with a 12-h light and dark cycle and fed Formulab Diet 5008. Age- (60-day) and glucose-matched male Zucker diabetic fatty rats are gavaged twice daily for 14 days with vehicle (0.05 M N-methylglucamine), GW1929 (0.5, 1.0, or 5.0 mg/kg), or troglitazone (as the milled extrudate, in a suspension in methylcellulose, 50, 150, and 500 mg/kg). Another group of animals receives a mixture of Humulin N and Humulin R by subcutaneous injection twice daily. On days 7 and 14 of dosing, nonfasted measurements of glucose, lactate, insulin, total cholesterol, TGs, F FAs, and hematocrit are obtained. On day 14 of dosing, samples for serum drug levels (2-h postdose) and glycosylated hemoglobin measurements are also collected. In addition, once weekly, three animals from each group are placed in metabolic chambers for 48 h for quantitation of 24-h food and water consumption. Body weights are recorded throughout the study. At the conclusion of the study, perfused pancreas experiments are performed on 12 animals (n = 4 per group) that have received either GW1929 (1 and 5 mg/kg) or vehicle, to directly evaluate the effects of treatment on basal and glucose-stimulated insulin secretion. The remaining animals are killed, and their pancreases are processed for immunocytochemistry [1]. |
| 体外活性 | GW1929是一种强效的PPAR-γ激活剂，对人类和小鼠的PPAR-γ的pEC50分别为8.56和8.27，同时对人类PPAR-γ、PPAR-α和PPAR-δ的pKis分别为8.84、小于5.5和小于6.5[1]。在浓度为10μM时，GW1929能够抑制TBBPA诱导的新皮层细胞培养中caspase-3的增加和TBBPA刺激的LDH释放[2]。 |
| 体内活性 | GW1929（0.5、1、5 mg/kg，p.o.）在治疗14天后显著降低了Zucker糖尿病肥胖（ZDF）大鼠的非空腹血糖水平，并具有抗脂解作用。在ZDF大鼠中，GW1929（1、5 mg/kg，p.o.）增强了β细胞对葡萄糖刺激的胰岛素分泌能力[1]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.04 mM), Sonication is recommended. DMSO : 33 mg/mL (66.59 mM), Sonication is recommended. |
| 关键字 | PPARγ | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibit | GW-1929 | GW1929 | GW 1929 |
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| 相关库 | Neuroprotective Compound Library | Lipid Metabolism Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Transcription Factor-Targeted Compound Library | Anti-Cardiovascular Disease Compound Library | Preclinical Compound Library | Anti-Hypertension Compound Library | Anti-Obesity Compound Library | Nuclear Receptor Compound Library | DNA Damage & Repair Compound Library | Covalent Inhibitor Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 GW1929【196808-24-9】
￥279 - 4944
