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L-165041

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产品编号 T7159Cas号 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。

L-165041
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L-165041

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纯度: 97.97%
产品编号 T7159Cas号 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。

规格价格库存数量
1 mg
¥ 186
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5 mg
¥ 413
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10 mg
¥ 732
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25 mg
¥ 1,370
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50 mg
¥ 2,230
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100 mg
¥ 3,560
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200 mg
¥ 4,970
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1 mL x 10 mM (in DMSO)
¥ 366
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产品介绍

生物活性
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].
化学信息
分子量402.44
分子式C22H26O7
CAS No.79558-09-1
SmilesCCCc1c(O)c(ccc1OCCCOc1ccc(OCC(O)=O)cc1)C(C)=O
密度1.222 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (124.24 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.4848 mL12.4242 mL24.8484 mL124.2421 mL
5 mM0.4970 mL2.4848 mL4.9697 mL24.8484 mL
10 mM0.2485 mL1.2424 mL2.4848 mL12.4242 mL
20 mM0.1242 mL0.6212 mL1.2424 mL6.2121 mL
50 mM0.0497 mL0.2485 mL0.4970 mL2.4848 mL
100 mM0.0248 mL0.1242 mL0.2485 mL1.2424 mL

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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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 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。
% DMSO
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%Tween 80
%ddH2O

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