GLUT4

GLUT4-IN-2 是一种特异性 GLUT4 抑制剂，抑制 GLUT1 和 GLUT4。GLUT4-IN-2 具有抗肿瘤活性，诱导细胞凋亡 (apoptosis) 和细胞周期停滞，可用于研究癌症。

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。

β-Aminopropionitrile (3-Aminopropionitrile) 是赖氨酰氧化酶的特异性抑制剂。

Karanjin 是干花豆中的主要活性呋喃黄酮醇成分，可通过细胞周期阻滞诱导癌细胞死亡，促进细胞凋亡，还通过提高AMPK 的方式诱导骨骼肌细胞 GLUT4 易位。

MitoPQ (MitoParaquat) 是一个线粒体靶向的小分子化合物。MitoPQ 选择性加强线粒体超氧化物和过氧化氢的含量，抑制胰岛素刺激的葡萄糖摄取和葡萄糖转运蛋白 4 (GLUT4） 向脂肪细胞和肌管中质膜的易位。MitoPQ 可用于研究线粒体氧化应激与调节的 GLUT4 转运。

Fasentin (N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide) 是葡萄糖摄取抑制剂，可抑制GLUT-1/GLUT-4转运蛋白，优先抑制 GLUT4，IC50为 68 μM。它是死亡受体刺激敏化剂，可敏化细胞对 FAS 诱导的细胞死亡，具有抗血管生成活性。

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。

GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).

GLUT4 activator3 (Compound 13a) 是一种用于骨骼肌中GLUT4转位的抗糖尿病药物。它能够促进骨骼肌细胞内葡萄糖转运蛋白4 (GLUT4) 的转位，并降低 STZ 诱导的糖尿病大鼠的血糖水平。

M617 acetate 是甘丙肽受体 1 (GAL1) 的选择性激动剂。 M617 acetate 通过中枢 GAL1 起作用，促进 GLUT4 表达，并提高 2 型糖尿病大鼠心肌中的 GLUT4 含量。 GAL1 和 GAL2 的 Ki 值分别为 0.23 和 5.71 nM。

DCW-234，作为一种ERbeta选择性激动剂，对ERbeta具有优于ERalpha的结合亲和力，能有效促进ERbeta/SRC1的强选择性相互作用。研究表明，DCW-234可以在CHO-K1细胞中诱导GLUT4的表达。

Antidiabetic agent 7 (Compound 5m) 是一种有效的高血糖抑制剂，能够通过激活AMPK依赖途径显著促进骨骼肌细胞中的GLUT4转运。它在降低血糖水平方面具有良好效果，并显示出优越的药代动力学特性，适用于抗高血糖研究。

Rapaglutin A 是一种葡萄糖转运蛋白 (GLUT) 抑制剂，它作为 I 类异构体 GLUT1、GLUT3 和 GLUT4 的泛GLUT抑制剂，IC50为 12 nM。Rapaglutin A 对 A549 细胞增殖具有抑制效果。

DS-1150b 是一种口服有效的GLUT4激活剂，能够激活GLUT4转运，促进骨骼肌细胞中GLUT4向细胞膜移位。在Zucker肥胖大鼠模型中，DS-1150b 显示出降血糖效果，可用于2型糖尿病 (T2DM) 的研究。

JTT-553 是一种 DGAT1 抑制剂 (IC50: 2.38 nM)。它可降低血浆中葡萄糖、胰岛素、非酯化脂肪酸 (NEFA)、总胆固醇 (TC) 和肝脏甘油三酯 (TG) 的浓度。在 DIO 小鼠中，JTT-553 改善了脂肪组织中胰岛素依赖性葡萄糖的摄取和葡萄糖不耐受的问题。此外，JTT-553 在 KK-Ay 小鼠中降低脂肪组织中的 TNF-α mRNA 水平，并提高 GLUT4 mRNA 的水平。通过减轻体重，JTT-553 改善了胰岛素抵抗和全身葡萄糖代谢。JTT-553 可用于研究肥胖症及 2 型糖尿病 (T2DM)。

VSP-77 是一种可口服的PPARγ激动剂。通过抑制CDK5介导的PPARγ在Ser-273位点的磷酸化，VSP-77 选择性上调与胰岛素敏感性相关的基因 (Glut4和Adiponectin) 的表达。在高脂饮食诱导的糖尿病小鼠模型中，VSP-77 显著改善葡萄糖耐量，降低空腹血糖和胰岛素水平，适用于糖尿病研究。

GTPγS (Guanosine 5'-[γ-thio]triphosphate) 是一种G蛋白激动剂，能够保护蛋白质免受蛋白水解，同时通过酪氨酸激酶依赖机制促进GLUT4的易位，刺激磷脂酶并诱导肌动蛋白的聚合。它与G蛋白α的结合可用于研究激酶活性，并可作为裂解缓冲液的成分。

HK2-IN-3 (compound 12) 是一种强效抑制己糖激酶 2 (HK2) 的化合物，表现出IC50为56.4 nM的效果。此化合物在口腔鳞状细胞癌 (OSCC) 中减少葡萄糖摄取，且下调GLUT1/GLUT4的表达，诱导线粒体自噬 (mitophagy) 和细胞凋亡 (apoptosis)。在OSCC异种移植小鼠模型中，HK2-IN-3 抑制肿瘤的生长和血管生成，可用于OSCC的研究。

Rhoifolin (Apigenin 7-O-neohesperidoside) 是从琯溪蜜柚叶子分离的一种黄酮糖苷。它通过 RANKL 诱导的NF-κB 和MAPK 途径改善钛颗粒刺激的骨溶解并减少破骨细胞生成。它通过增强脂联素分泌，胰岛素受体-β的酪氨酸磷酸化和GLUT4易位有助于治疗糖尿病并发症。

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).

10-PAHSA is a newly identified endogenous lipid that belongs to a collection of branched fatty acid esters of hydroxy fatty acids (FAHFAs). It is a FAHFA in which palmitic acid is esterified to 10-hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. As other FAHFAs improve glucose tolerance, stimulate insulin secretion, and have anti-inflammatory effects, 10-PAHSA may be a bioactive lipid with roles in metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to either a C-16 or C-18 hydroxy substituent. 12-PAHSA is a FAHFA in which palmitic acid is esterified at the 12th carbon of hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. 12-PAHSA is present at 2- to 3-fold higher levels in adipose tissue of AG4OX mice compared to wild type mice. Levels of 12-PAHSA are also higher in fasted wild-type mice compared to fed mice and are reduced upon high-fat diet-induced obesity in insulin-resistant mice.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to a hydroxylated C-16 or C-18 lipid. 9-PAHSA is a FAHFA in which palmitic acid is esterified to 9-hydroxy stearic acid. PAHSAs are the most abundant forms of FAHFA in serum as well as white and brown adipose tissues of glucose tolerant AG4OX mice, which overexpress Glut4 specifically in adipose tissue. 9-PAHSA is the predominant isomer of PAHSA in wild type and AG4OX mice. It is found in humans and is reduced in the serum and adipose tissues of insulin-resistant humans. 9-PAHSA improves glucose tolerance, stimulates insulin secretion, and has anti-inflammatory effects in mice.

Apigenin 7-glucoside (Cosmosiin) 是一种 ROS 清除剂，具有抗增殖、抗氧化作用。