L-165041
基本信息
产品名称：
L-165041
英文名称：
L-165041
国产/进口：
进口
产地/品牌：
美国/TargetMol
型号：
参考报价：
面议
销售商：
总点击数：
36
更新日期：
2025-05-27
产品类别：
性能参数
Product Introduction
Bioactivity
英文名: L-165041
描述: 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。
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].
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].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (124.24 mM)
关键字: L 165041 | Peroxisome proliferator-activated receptors | PPAR | L-165041 | L165041 | inhibit | Inhibitor
相关产品: Foenumoside B | Glycyrin | Alpinetin | Seratrodast | Mifobate | Furegrelate | Uvaol | Glipizide | KD-3010 | BAY-0069
相关库: Anti-COVID-19 Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Anti-Obesity Compound Library | Lipid Metabolism Compound Library | DNA Damage & Repair Compound Library | Metabolism Compound Library | NO PAINS Compound Library
Bioactivity
英文名: L-165041
描述: 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。
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].
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].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (124.24 mM)
关键字: L 165041 | Peroxisome proliferator-activated receptors | PPAR | L-165041 | L165041 | inhibit | Inhibitor
相关产品: Foenumoside B | Glycyrin | Alpinetin | Seratrodast | Mifobate | Furegrelate | Uvaol | Glipizide | KD-3010 | BAY-0069
相关库: Anti-COVID-19 Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Anti-Obesity Compound Library | Lipid Metabolism Compound Library | DNA Damage & Repair Compound Library | Metabolism Compound Library | NO PAINS Compound Library
公司简介
TargetMol（陶术）作为一家全球性的生物医药领域高科技企业，我们致力于为高校、研究所、医院、企业等各类生物医药研发机构提供优质的产品和服务，为全球医药科学家更高效地完成科研工作助力。可提供20,000+种 抑制剂和激动剂 、800+种 化合物库 、19,000+种 天然产物 ，以及9,000+种 重组蛋白 、多种 多肽 、抗体 和 生命科学试剂盒 等。此外，在上海，TargetMol研发中心配备了 CADD & AIDD研究中心、药理实验室和药物化学合成 平台三大技术中心，可提供虚拟筛选、化合物活性测试、分子间结合力检测和化合物结构优化等技术服务，多方位满足用户的研发需求。
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