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L-165041

L-165041

产品编号 T7159   CAS 79558-09-1

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。

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L-165041 Chemical Structure
L-165041, CAS 79558-09-1
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
产品目录号及名称: L-165041 (T7159)
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (124.24 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Park J H , Lee K S , Lim H J , et al. The PPARδ ligand L-165041 inhibits vegf-induced angiogenesis, but the antiangiogenic effect is not related to PPARδ[J]. Journal of Cellular Biochemistry, 2012, 113(6):1947-1954. 2. Lim H J , Park J H , Lee S , et al. PPARδ ligand L-165041 ameliorates Western diet-induced hepatic lipid accumulation and inflammation in LDLR?/? mice[J]. European Journal of Pharmacology, 2009, 622(1-3):45-51.
GW590735 Ragaglitazar DSO-5a PPARγ agonist 8 Pioglitazone hydrochloride Sulotroban potassium Dihydrocurcumin Seladelpar

相关化合物库

该产品包含在如下化合物库中:
抗糖尿病库 经典已知活性库 干细胞分化化合物库 DNA 损伤和修复分子库 代谢化合物库 转录因子库 抗高血压化合物库 抗胰腺癌化合物库 糖代谢化合物库 NO PAINS 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

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。

Keywords

L-165041 79558-09-1 DNA Damage/DNA Repair Metabolism PPAR L 165041 Peroxisome proliferator-activated receptors L165041 inhibit Inhibitor inhibitor

 

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