5-[(2,4-二氧代噻唑啉-5-基)甲基]-2-甲氧基-N-[[4-(三氟甲基)苯基]甲基]苯甲酰胺

• 常用名: 5-[(2,4-二氧代噻唑啉-5-基)甲基]-2-甲氧基-N-[[4-(三氟甲基)苯基]甲基]苯甲酰胺
• 英文名: KRP-297
• CAS号: 213252-19-8
• 分子量: 438.42000
• 密度: 1.395g/cm3
• 沸点: 605.4ºC at 760 mmHg
• 分子式: C₂₀H₁₇F₃N₂O₄S
• 熔点: N/A
• 闪点: 319.9ºC

用途

KRP-297是一种PPARα和PPARγ激动剂,可能用于治疗2型糖尿病和血脂异常。KRP-297可恢复降低的脂质氧化,并抑制肝脏中增强的脂肪生成和甘油三酯积累。

名称

• 中文名: 5-[(2,4-二氧代噻唑啉-5-基)甲基]-2-甲氧基-N-[[4-(三氟甲基)苯基]甲基]苯甲酰胺
• 英文名: 5-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide

生物活性

• 描述: KRP-297是一种PPARα和PPARγ激动剂,可能用于治疗2型糖尿病和血脂异常。KRP-297可恢复降低的脂质氧化,并抑制肝脏中增强的脂肪生成和甘油三酯积累。
• 相关类别:
  信号通路 >> 细胞周期/DNA损伤 >> PPAR
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. Murakami K, Tobe K, Ide T, et al. A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats. Diabetes. 1998;47(12):1841-1847.

  [2]. Kochansky CJ, Rippley RK, Yan KX, et al. Absorption, metabolism, and excretion of [14C]MK-0767 (2-methoxy-5-(2,4-dioxo-5-thiazolidinyl)-N-[[4-(trifluoromethyl)phenyl] methyl]benzamide) in humans. Drug Metab Dispos. 2006;34(9):1457-1461.

物理化学性质

• 密度: 1.395g/cm3
• 沸点: 605.4ºC at 760 mmHg
• 分子式: C₂₀H₁₇F₃N₂O₄S
• 分子量: 438.42000
• 闪点: 319.9ºC
• 精确质量: 438.08600
• PSA: 116.78000
• LogP: 4.38880
• InChIKey: NFFXEUUOMTXWCX-UHFFFAOYSA-N
• SMILES: COc1ccc(CC2SC(=O)NC2=O)cc1C(=O)NCc1ccc(C(F)(F)F)cc1
• 蒸汽压: 1.32E-14mmHg at 25°C
• 折射率: 1.58

靶点实验

查看更多实验

实验名称：Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro... 来源：NCGC 靶标：N/A External Id：SERCaMPGLuc-p1-antagonist

实验名称：Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression 来源：NCGC External Id：SNCA-p-activity-luciferase

实验名称：Primary qHTS for Identification of Small Molecule Activators of Huntingtin-Antisense ... 来源：NCGC External Id：huntington-HTTAS8-p1-FF-overN

实验名称：Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Ga... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor gamma External Id：CHEMBL1781231

实验名称：Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Ga... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor alpha External Id：CHEMBL1781230

实验名称：Binding affinity for human peroxisome proliferator activated receptor gamma 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor gamma External Id：CHEMBL841786

实验名称：Induction of oligodendrocyte precursor cell differentiation isolated from Wistar rat ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL1781233

实验名称：Binding affinity for human peroxisome proliferator activated receptor alpha 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor alpha External Id：CHEMBL841785

实验名称：Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Ga... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor delta External Id：CHEMBL1781232

实验名称：Agonist activity at GAL4-fused PPARalpha assessed as transcriptional activity by cell... 来源：ChEMBL 靶标：Peroxisome proliferator-activated receptor alpha External Id：CHEMBL2216559

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英文别名

• [3H]-MK-0767
• N-(4-trifluoromethylbenzyl)-5-(2,4-dioxothiazolidin-5-yl)methyl-2-methoxybenzamide
• [14C]-MK-0767
• 5-((2,4-Dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide
• 5-(2,4-dioxothiazolidin-5-ylmethyl)-2-methoxy-N-[4-(trifluoromethyl)benzyl]benzamide
• MK 767
• MK-0767
• 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide
• KRP 297