Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10507 |
GPR40 Agonist 2
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
GPR40 Agonist 2 is a GPR40 agonist. It can be used in the research of diabetes. | |||
T15810 |
LY2922470
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GPR | Endocrinology/Hormones; GPCR/G Protein |
LY2922470 是选择性口服有效的GPR40激动剂,作用于 人 GPR40、小鼠 GPR40、大鼠 GPR40 的EC50值分别为 7 nM、1 nM、3 nM。它可降低血糖水平,同时显著增加胰岛素和 GLP-1,有潜力用于 2 型糖尿病的研究。 | |||
T60184 |
TUG-499
|
GPR; PPAR | DNA Damage/DNA Repair; Endocrinology/Hormones; GPCR/G Protein; Metabolism |
TUG-499 是一种选择性游离脂肪酸受体 1 (FFAR1 或 GPR40)激动剂(EC50 : 7.39)。TUG-499对 FFAR1 或 GPR40的亲和力超过相关受体 FFA2、FFA3 和核受体 PPARγ,以及其他不同的受体、离子通道和转运蛋白。TUG-499 可用于研究 2 型糖尿病。 | |||
T62542 |
GPR40 agonist 5
|
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GPR40 agonist 5 是一种口服具有活力的 GPR40 (G 蛋白偶联受体 40) 激动剂 (EC50: 47 nM)。GPR40 agonist 5 能够减少血糖水平,改善糖耐量。GPR40 agonist 5 对 2 型糖尿病小鼠的高血糖状态表现出充足的控制作用。 | |||
T11459 |
GPR40 agonist 1
|
Others | Others |
GPR40 agonist 1 is an effective new GPR40 agonist (EC50s: 17 nM and 2 nM for rGPR40 and hGPR40). | |||
T14202 | AM-4668 | GPR | Endocrinology/Hormones; GPCR/G Protein |
AM-4668 is a type 2 diabetes GPR40 agonist. For GPR40, in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), the EC50s are 3.6 nM and 36 nM, respectively. | |||
T69953 | MK-8666 Tris | ||
MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects. | |||
T70468 | MK-8666 | ||
MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects. | |||
T73434 |
BI-2081
|
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BI-2081是一种GPR40 (FFAR1)部分激动剂,具有EC50值为4 nM。该化合物能诱导葡萄糖依赖性胰岛素释放,并降低血浆中葡萄糖含量,适用于研究代谢疾病,尤其是2型糖尿病。 | |||
T36634 |
ZQ 16
|
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Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characte... | |||
T35816 |
ZLY032
|
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ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic st... |