LY518674

• 常用名: LY518674
• 英文名: LY518674
• CAS号: 425671-29-0
• 分子量: 409.47800
• 密度: 1.21g/cm3
• 沸点: 575.852ºC at 760 mmHg
• 分子式: C₂₃H₂₇N₃O₄
• 熔点: N/A
• 闪点: 302.065ºC

LY518674用途

LY518674 是高效、选择性的 PPARα 拮抗剂,对人 human PPARα 作用的 EC50 值为 42 nM。LY518674 能降低甘油三酸酯,增加 HDL-C,可用于治疗动脉粥样硬化。

LY518674名称

• 中文名: 2-[4-[3-[2,5-二氢-1-[(4-甲基苯基)甲基]-5-氧代-1H-1,2,4-T噻唑-3-基]丙基]苯氧基]-2-甲基-丙酸
• 英文名: 2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid

LY518674生物活性

• 描述: LY518674 是高效、选择性的 PPARα 拮抗剂,对人 human PPARα 作用的 EC50 值为 42 nM。LY518674 能降低甘油三酸酯,增加 HDL-C,可用于治疗动脉粥样硬化。
• 相关类别:
  信号通路 >> 细胞周期/DNA损伤 >> PPAR
  研究领域 >> 代谢疾病
• 靶点实验:

  EC50: 42 nM (human PPARα)[1]

• 体内研究: LY518674在体内降低甘油三酯和增加HDL-C[2]。LY518674显著提高载脂蛋白A-I(apoA-I)的转化率,但对载脂蛋白A-I或高密度脂蛋白胆固醇(HDL-C)的稳态水平无重大影响[3]。
• 参考文献:

  [1]. Bravo Y, et al. Identification of the first potent, selective and bioavailable PPARα antagonist. Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72.

  [2]. Nissen SE, et al. Effects of a potent and selective PPAR-alpha agonist in patients with atherogenic dyslipidemia or hypercholesterolemia: two randomized controlled trials. JAMA. 2007 Mar 28;297(12):1362-73.

  [3]. Khera AV, et al. Potent peroxisome proliferator-activated receptor-α agonist treatment increases cholesterol efflux capacity in humans with the metabolic syndrome. Eur Heart J. 2015 Nov 14;36(43):3020-2.

LY518674物理化学性质

• 密度: 1.21g/cm3
• 沸点: 575.852ºC at 760 mmHg
• 分子式: C₂₃H₂₇N₃O₄
• 分子量: 409.47800
• 闪点: 302.065ºC
• 精确质量: 409.20000
• PSA: 97.21000
• LogP: 3.34540
• 折射率: 1.594
• 储存条件: 2-8°C

LY518674靶点实验

查看更多实验

实验名称：Cotransfection activity against human Peroxisome proliferator activated receptor alph... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor alpha External Id：CHEMBL760605

实验名称：Compound was evaluated in human apoA-I transgenic mice for maximal percent increase i... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL721333

实验名称：Compound was evaluated in human apoA-I transgenic mice for its ability to alter serum... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL722168

实验名称：Compound was evaluated in human apoA-I transgenic mice for its ability to alter HDL-c... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL722167

实验名称：Human Peroxisome proliferator-activated receptor-alpha (1C. Peroxisome proliferator-a... 来源：IUPHAR-DB 靶标：Peroxisome proliferator-activated receptor-alpha (1C. Peroxisome proliferator-activated receptors) [Homo sapiens] External Id：593_Human

实验名称：Agonist activity at PPARalpha 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor alpha External Id：CHEMBL2038446

实验名称：Agonist activity at PPARdelta 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor delta External Id：CHEMBL2038596

实验名称：Agonist activity at PPARgamma 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor gamma External Id：CHEMBL2038597

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LY518674英文别名

• 2-Methyl-2-[4-[3-[1-(4-Methylbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl]propyl]phenoxy]propionic acid
• Propanoic acid,2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl
• 2-[4-[3-[4,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
• 2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl-propanoic acid