SSTR5拮抗剂1

• 常用名: SSTR5拮抗剂1
• 英文名: SSTR5 antagonists 1
• CAS号: 1628741-91-2
• 分子量: 511.59
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₈H₃₄FN₃O₅
• 熔点: N/A
• 闪点: N/A

SSTR5拮抗剂1用途

SSTR5 antagonists 1是一种有效,选择性,可口服的生长抑素受体亚型5 (SSTR5) 拮抗剂,对hSSTR5和mSSTR5的 IC50 分别为9.6和 57 nM。 (化合物25a)

SSTR5拮抗剂1名称

• 中文名: SSTR5拮抗剂1
• 英文名: SSTR5 antagonists 1

SSTR5拮抗剂1生物活性

• 描述: SSTR5 antagonists 1是一种有效,选择性,可口服的生长抑素受体亚型5 (SSTR5) 拮抗剂,对hSSTR5和mSSTR5的 IC50 分别为9.6和 57 nM。 (化合物25a)
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 生长抑素受体
  研究领域 >> 代谢疾病
• 靶点实验:

  IC50: 9.6 nM (hSSTR5), 57 nM (mSSTR5)[1]

• 参考文献:

  [1]. Hirose H, et al. Discovery of novel 5-oxa-2,6-diazaspiro[3.4]oct-6-ene derivatives as potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonists for treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2017 Aug 1;25(15):4175-4193.

SSTR5拮抗剂1物理化学性质

• 分子式: C₂₈H₃₄FN₃O₅
• 分子量: 511.59
• InChIKey: UQRAIIGEZLINAT-UHFFFAOYSA-N
• SMILES: CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1

SSTR5拮抗剂1靶点实验

查看更多实验

实验名称：Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as decrease in blood glucose... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4056248

实验名称：Antidiabetic activity in HFD-fed SSTR5 knockout C57BL/6J mouse assessed as decrease i... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4056249

实验名称：Mean residence time in ICR mouse at 0.1 mg/kg, iv administered as cassette dose by LC... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4056232

实验名称：Total clearance in ICR mouse at 0.1 mg/kg, iv administered as cassette dose by LC/MS/... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4056230

实验名称：Volume of distribution at steady state in ICR mouse at 0.1 mg/kg, iv administered as ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4056231

实验名称：Intrinsic clearance in mouse liver microsomes at 1 uM after 15 to 30 mins in presence... 来源：ChEMBL 靶标：Liver External Id：CHEMBL4056228

实验名称：Solubility of the compound in aqueous buffer solution at pH 6.8 after 18 hrs by HPLC ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4056229

实验名称：Inhibition of human SSTR4 at 10 uM by radioligand binding assay relative to control 来源：ChEMBL 靶标：Somatostatin receptor type 4 External Id：CHEMBL4056226

实验名称：Intrinsic clearance in human liver microsomes at 1 uM after 15 to 30 mins in presence... 来源：ChEMBL 靶标：Liver External Id：CHEMBL4056227

实验名称：Antidiabetic activity in HFD-fed C57BL/6J mouse assessed as decrease in blood glucose... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4056241

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