glut2

BAY-876 是一种葡萄糖转运蛋白 1 (GLUT1) 抑制剂 (IC50=2 nM)，具有口服活性和选择性。BAY-876 对 GLUT1 选择性比 GLUT2、GLUT3 和 GLUT4 高 100 倍以上。BAY-876 抑制糖酵解代谢，具有抗肿瘤活性。

(−)-Myrtenal 是一种具有口服活性及抗肿瘤活性的萜烯。(-)-Myrtenal 作用于糖尿病大鼠的骨骼肌和肝脏，利用 Akt 增强 GLUT2 ，进而改善高血糖症。

KL-11743 是葡萄糖竞争性 I 类葡萄糖转运蛋白抑制剂，口服有活性，能够抑制GLUT1 (IC50:115 nM) 、GLUT2 (IC50:137 nM) 、GLUT3 (IC50:90 nM) 及GLUT4 (IC50:68 nM) 。它能够特异性阻断葡萄糖代谢，也可与电子传递抑制剂协同作用诱导细胞死亡。

T-1095 是一种口服有活性的Na+-葡萄糖协同转运蛋白选择性抑制剂，能够抑制 SGLT1 (IC50:22.8 µm) 及 SGLT2 (IC50:2.3 µm) 。它可用于研究糖尿病。

G2iA 是一种新型的高效 GLUT2-选择性抑制剂，其半抑制浓度 (IC50) 为0.61 µM。

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019). MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice. References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019).