1. GPCR/G Protein
  2. G Protein-coupled Receptor Kinase (GRK)
  3. DS-1558

DS-1558 是具有口服活性的 G protein-coupled receptor 40 激动剂。DS-1558 不仅增加了胰高血糖素样肽-1 (GLP-1) 促进的葡萄糖刺激胰岛素分泌,而且在正常 Sprague Dawley 大鼠中增强了静脉注射葡萄糖后的 GLP-1 最大胰岛素生成效应。DS-1558 有望用于 2 型糖尿病的研究。

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DS-1558

DS-1558 Chemical Structure

CAS No. : 1202575-67-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DS-1558 is an orally active small molecule G protein-coupled receptor 40 agonist. DS-1558 not only increases the glucose-stimulated insulin secretion by glucagon like peptide-1 (GLP-1) but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats. DS-1558 is promising for research of type 2 diabetes[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
11 nM
Compound: 29r, DS-1558
Agonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
Agonist activity at rat GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
[PMID: 26234904]
CHO EC50
3.7 nM
Compound: 13, DS-1558
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
Agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by FLIPR assay
[PMID: 25815144]
CHO EC50
3.7 nM
Compound: 29r, DS-1558
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular calcium level after 60 mins by FLIPR assay
[PMID: 26234904]
分子量

394.38

Formula

C21H21F3O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
DS-1558
目录号:
HY-12976
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