AS1269574

• 常用名: AS1269574
• 英文名: AS 1269574
• CAS号: 330981-72-1
• 分子量: 308.174
• 密度: 1.5±0.1 g/cm3
• 沸点: 386.9±42.0 °C at 760 mmHg
• 分子式: C₁₃H₁₄BrN₃O
• 熔点: N/A
• 闪点: 187.8±27.9 °C

AS1269574用途

AS1269574 是一种有效的,具有口服活性的 GPR119 激动剂,在表达人 GPR119 的 HEK293 细胞中 EC50 为 2.5 μM。AS1269574 激活 TRPA1 阳离子通道,刺激胰高血糖素样肽-1 (GLP-1) 分泌。AS1269574 仅在高糖条件下特异性诱导胰腺 β 细胞分泌葡萄糖依赖性胰岛素。AS1269574 对 2 型糖尿病研究具有潜力。

AS1269574名称

• 中文名: AS1269574
• 英文名: 2-[[2-(4-bromophenyl)-6-methylpyrimidin-4-yl]amino]ethanol

AS1269574生物活性

• 描述: AS1269574 是一种有效的,具有口服活性的 GPR119 激动剂,在表达人 GPR119 的 HEK293 细胞中 EC50 为 2.5 μM。AS1269574 激活 TRPA1 阳离子通道,刺激胰高血糖素样肽-1 (GLP-1) 分泌。AS1269574 仅在高糖条件下特异性诱导胰腺 β 细胞分泌葡萄糖依赖性胰岛素。AS1269574 对 2 型糖尿病研究具有潜力。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GPR119
  研究领域 >> 代谢疾病
• 靶点实验:

  TRPA1

  GPR119

• 体内研究: AS1269574可显著降低给药2小时(AUC0-2小时)后的血糖AUC[1]。动物模型：8周龄ICR小鼠[1]剂量：100mg/kg给药：P.o.结果：给药2h(AUC0-2h)后,血糖AUC明显降低。同样,小鼠血浆胰岛素AUC0-2h也显著升高。
• 参考文献:

  [1]. Yoshida S, et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem Biophys Res Commun. 2010;400(3):437-441.

  [2]. Chepurny OG, et al. GPR119 Agonist AS1269574 Activates TRPA1 Cation Channels to Stimulate GLP-1 Secretion. Mol Endocrinol. 2016;30(6):614-629.

AS1269574物理化学性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 386.9±42.0 °C at 760 mmHg
• 分子式: C₁₃H₁₄BrN₃O
• 分子量: 308.174
• 闪点: 187.8±27.9 °C
• 精确质量: 307.032013
• PSA: 58.04000
• LogP: 2.32
• InChIKey: DUKPGOOUJNUIOI-UHFFFAOYSA-N
• SMILES: Cc1cc(NCCO)nc(-c2ccc(Br)cc2)n1
• 外观性状: 琥珀色的固体
• 蒸汽压: 0.0±0.9 mmHg at 25°C
• 折射率: 1.648
• 储存条件: -20℃

AS1269574靶点实验

查看更多实验

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：Antihyperglycemic activity in ICR mouse assessed as blood glucose lowering ratio at 3... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL1958727

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Chemical Probes of Kaposi's Sarcoma Herpes Virus Latent Infection 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：ORF 73 [Human herpesvirus 8 type M] External Id：HMS791

实验名称：Antihyperglycemic activity in ICR mouse assessed as blood glucose lowering ratio at 1... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL1958726

实验名称：Hit confirmation of the active molecules of the enzymatic assay of human HDAC6 with c... 来源：ChEMBL 靶标：Histone deacetylase 6 External Id：CHEMBL4808151

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4303805

实验名称：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

实验名称：A screen for compounds that inhibit viral RNA polymerase binding and polymerization a... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Chain A, Poliovirus Polymerase With Gtp External Id：HMS750

共15条，当前第1页，共2页

1

2

AS1269574英文别名

• hms1581i01
• 2-{[2-(4-Bromophenyl)-6-methyl-4-pyrimidinyl]amino}ethanol
• AS-1269574