Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T62856 |
FFA1 agonist-1
|
Others | Others |
FFA1 agonist-1 (Compound 17a) 是一种口服具有活力的脂肪酸受体(FFA1)激动剂 (EC50: 0.75 μM)。FFA1 agonist-1 能够用于研究 Ⅱ 型糖尿病。 | |||
TQ0020 |
AMG 837 calcium hydrate
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
AMG 837 calcium hydrate 是口服有效的 GPR40/FFA1部分激动剂,抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合,pIC50为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。 | |||
T3171 |
GSK137647A
GSK 137647 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
GSK137647A (GSK 137647) 是一种选择性FFA4激动剂,作用于人类和大小鼠FFA4的pEC50分别为6.3、6.1和6.2。 | |||
T1781 |
GW9508
GW 9508 |
GPR; Potassium Channel | Endocrinology/Hormones; GPCR/G Protein; Membrane transporter/Ion channel |
GW 9508 是一种选择性 G 蛋白偶联受体FFA1(GPR40) 和GPR120激动剂。它是一种葡萄糖敏感性胰岛素促分泌剂和 ATP 敏感性钾通道开放剂,具有抗炎和抗动脉粥样硬化活性。 | |||
TQ0241 |
TUG-770
TUG770,TUG 770 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
TUG-770 是一种具有口服活性、选择性和高效性的 GPR40/FFA1 激动剂,具有潜在的抗炎活性。TUG-770 可用于研究 2 型糖尿病、痴呆和阿尔茨海默症。 | |||
T17177 |
TUG-424
TUG424 |
Others | Others |
TUG-424 是一种有效且选择性的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂,EC50 为 32 nM。TUG-424 在 100 nM 处显著增加葡萄糖刺激的胰岛素分泌。TUG-424 可能有助于探索 FFA1 在糖尿病或肥胖等代谢性疾病中的作用。 | |||
T7127 |
DC260126
|
Apoptosis; GPR | Apoptosis; Endocrinology/Hormones; GPCR/G Protein |
DC260126 是一种 GPR40 (FFAR1)拮抗剂,对棕榈酸酯诱导的内质网应激和凋亡有保护作用。它剂量依赖性地抑制亚油酸、油酸、棕榈油酸和月桂酸刺激的 GPR40 介导的 Ca2+升高,IC50分别 6.28、5.96、7.07和4.58 μM。 | |||
T22967 |
MEDICA16
MEDICA 16 |
GPR; Others; ATP Citrate Lyase | Endocrinology/Hormones; GPCR/G Protein; Metabolism; Others |
MEDICA16 是 GPR40 的特异性激动剂以及 GPR120 的部分激动剂。 MEDICA16 是一种 ATP-柠檬酸裂解酶抑制剂,可显着降低腓肠肌中的细胞内 TG 含量,同时增加胰岛素敏感性。 | |||
T14200 | AM-1638 | GPR | Endocrinology/Hormones; GPCR/G Protein |
AM-1638 is a full agonist of GPR40/FFA1 (EC50: 0.16 μM). | |||
T2351 |
Fasiglifam
TAK875 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
Fasiglifam (TAK875) 是一种可口服的选择性GPR40激动剂,EC50值为 72 nM。 | |||
T15448 |
GW-1100
GW 1100,GW1100 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
GW-1100是选择性的 GPR40 和 FFAR1 拮抗剂,可用于研究糖尿病和代谢疾病。 | |||
T15810 |
LY2922470
|
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。 | |||
T62848 |
AMG 837 hemicalcium
|
Others | Others |
AMG 837 hemicalcium 是一种有效的、口服具有活力的 GPR40/FFA1部分激动剂。AMG 837 hemicalcium 能够抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合 (pIC50: 8.13)。AMG 837 hemicalcium 能够提高啮齿动物的胰岛素分泌,减少葡萄糖水平。 | |||
T11583 |
HWL-088
|
Others | Others |
HWL-088 is a potent free fatty acid receptor 1 (FFA1/GPR40) agonist. HWL-088 significantly improves glucose tolerance in normal and diabetic models. | |||
T35816 |
ZLY032
|
Others | Others |
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... | |||
T26868 |
BMS-986118
BMS 986118 |
Others | Others |
BMS-986118 is a full agonist of GPR40, is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial a | |||
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. | |||
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). | |||
T2351L |
TAK-875 Hemihydrate
TAK-875,Fasiglifam |
GPR | Endocrinology/Hormones; GPCR/G Protein |
TAK-875 Hemihydrate (Fasiglifam) 是一种选择性 GPR40 激动剂,EC50 为 14 nM,比油酸强 400 倍。 | |||
T13550 |
AP5
|
Others | Others |
AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor. |