Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L-165041 是一种细胞渗透性 PPARδ激动剂,可在 NIH-PPARδ 细胞中诱导脂肪细胞分化,对 PPARδ 和 PPARγ 的 Ki 值分别为 6 nM 和 约 730 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 297 | 现货 | ||
5 mg | ¥ 490 | 现货 | ||
10 mg | ¥ 733 | 现货 | ||
25 mg | ¥ 1,480 | 现货 | ||
50 mg | ¥ 2,930 | 现货 | ||
100 mg | ¥ 4,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 548 | 现货 |
产品描述 | L-165041 is a potent and selective agonist of the nuclear receptor PPARβ and PPARδ(Ki = 9 nM, EC50 = ~500 nM ,respectively) |
靶点活性 | PPARδ:500 nM(EC50), PPARβ:9 nM(ki) |
体外活性 | L-165041 inhibited VEGF-induced cell proliferation and migration in human umbilical vein ECs (HUVECs). L-165041 also inhibited angiogenesis in the Matrigel plug assay and aortic ring assay. Flow cytometric analysis indicated that L-165041 reduced the number of ECs in the S phase and the expression levels of cell cycle regulatory proteins such as cyclin A, cyclin E, CDK2, and CDK4; phosphorylation of the retinoblastoma protein was suppressed by pretreatment with L-165041. The PPARδ ligand L-165041 inhibits VEGF-stimulated angiogenesis by suppressing the cell cycle progression independently of PPARδ[1]. |
体内活性 | L-165041 lowered hepatic expression of PPARgamma, apolipoprotein B, interleukin 1 beta (IL-1beta), and interleukin-6. In contrast, L-165041 increased hepatic expressions of PPARdelta, lipoprotein lipase (LPL), and ATP-binding cassette transporter G1 (ABCG1).L-165041 might be effective in preventing Western diet-induced hepatic steatosis by regulating genes involved in lipid metabolism and the inflammatory response[2]. |
细胞实验 | Cell cycle distribution was determined by flow cytometry. Synchronized HUVECs were pretreated with L-165041 (1 or 5μM) 6 h prior to the addition of VEGF (10 ng/ml). The cells were harvested 16 h after VEGF addition and washed with PBS. The cells were then incubated with buffer containing 0.1% Triton X-100 and 0.1% trisodium citrate for 30 min. Cells were rinsed with PBS and then stained with 50 μg/ml propidium iodide for 20 min at room temperature. In total, 1*10^4 cells were analyzed with the FACScan system . At least three independent experiments were performed[1]. |
动物实验 | The effect of PPARdelta ligand L-165041 on Western diet-induced fatty liver using low-density lipoprotein receptor-deficient (LDLR(-/-)) mice. LDLR(-/-) mice received either L-165041 (5mg/kg/day) or vehicle (0.1N NaOH) with Western diet for 16 weeks. L-165041 drastically reduced lipid accumulation in the liver, decreasing total hepatic cholesterol and triglyceride content compared to the vehicle group[1]. |
分子量 | 402.44 |
分子式 | C22H26O7 |
CAS No. | 79558-09-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (124.24 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4848 mL | 12.4242 mL | 24.8484 mL | 62.1211 mL |
5 mM | 0.497 mL | 2.4848 mL | 4.9697 mL | 12.4242 mL | |
10 mM | 0.2485 mL | 1.2424 mL | 2.4848 mL | 6.2121 mL | |
20 mM | 0.1242 mL | 0.6212 mL | 1.2424 mL | 3.1061 mL | |
50 mM | 0.0497 mL | 0.2485 mL | 0.497 mL | 1.2424 mL | |
100 mM | 0.0248 mL | 0.1242 mL | 0.2485 mL | 0.6212 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。
L-165041 79558-09-1 DNA Damage/DNA Repair Metabolism PPAR L 165041 Peroxisome proliferator-activated receptors L165041 inhibit Inhibitor inhibitor