obese

FOY 251 是一种蛋白酶抑制剂，是具有抗蛋白水解活性的 Camostate 代谢物，能抑制 SARS-CoV-2 的感染。

ACH-000143 是一种可口服的褪黑素受体激动剂，对 MT1 和 MT2 的EC50值分别为0.06 和0.32 nM。

Ketoprofen (RP-19583) 是一种非甾体抗炎剂，能够有效地抑制COX 的活性，在人血单核细胞中，对 COX-1 和 COX-2 的IC50值分别为 2 nM 和 26 nM。

ML351 是一种高度特异的15-LOX-1抑制剂，其 IC50=200 nM。它对 T1D 非肥胖糖尿病小鼠模型的血糖异常和β细胞氧化应激有抑制作用。它对相关同工酶 (5-LOX、血小板 12-LOX、15-LOX-2、绵羊 COX-1 和人 COX-2) 表现出良好的选择性(>250倍)。

Cevoglitazar (LBM-642) 是一种 PPARɑ 激动剂和 PPARγ激动剂。Cevoglitazar 能有效减少肥胖小鼠和猴的食物摄入量和体重。

Emodin (Frangula emodin) 是 11β-HSD1 抑制剂，对人和小鼠 11β-HSD1 的 IC50 分别为 186 和 86 nM，具有选择性。Emodin 具有抗病毒、抗炎、抗癌作用。Emodin 可改善饮食诱导的肥胖小鼠的代谢紊乱。

Oxfenicine (4-Hydroxy-L-phenylglycine) 是具有口服活性的肉碱棕榈酰转移酶-1 抑制剂。它在缺血期间保护心脏免受坏死组织的损害。它可抑制心脏中脂肪酸的氧化。

CLT-28643是一种有效和特异性的α5β1-Integrin抑制剂，能够预防青光眼滤过手术（GFS）的纤维化，抑制肿瘤生长和血管生成，在博来霉素诱导的肺纤维化模型中抑制纤维化和炎症，改善肥胖小鼠H9C2细胞的胰岛素敏感性和心脏功能。

13-Oxo-9E,11E-octadecadienoic acid, a potent PPARα activator derived from tomato juice and an isomer of 9-oxo-ODA, exhibits the ability to decrease plasma and hepatic triglyceride levels in obese diabetic mice[1].

BRL 37344 sodium is a specific agonist of the β3-adrenergic receptor. The treatment of BRL 37344 sodium significantly lowers the bodyweight of obese mice.

D5D-IN-326 is an orally active delta-5 desaturase (D5D) inhibitor (IC50s: 72 and 22 nM for rat and human D5D in enzymic and cell-based assays). It has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in die

L 152804 是神经肽 Y Y5 受体的特异性拮抗剂，可调节食物摄入和能量消耗，从而导致饮食诱导的肥胖小鼠体重减轻。

α-Cyclodextrin (Alfadex) 是一种多功能可溶性膳食纤维，可作为纤维原料销售。

EB1002 是一种选择性NK2R激动剂，能够显著增加肥胖小鼠中线粒体生物合成相关基因（如PGC-1α）的表达，从而通过增强线粒体活动促进能量消耗。此外，它还提高了小鼠的胰岛素敏感性，并改善了糖脂代谢。因此，EB1002 有望用于针对肥胖和2型糖尿病的研究。

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)。

β-Hydroxybutyrate phenylalanine (BHB-Phe) 是一种次级酮体代谢物，由 β-hydroxybutyrate (BHB) 与必需氨基酸 L-phenylalanine 结合而成。它通过细胞质非特异性肽酶 2 (CNDP2) 在生酮作用后内源性形成。BHB-Phe (50 mg/kg 每天) 可在不影响活动、氧气消耗 (VO2) 或二氧化碳生成 (VCO2) 的情况下，减少饮食诱导肥胖 (DIO) 小鼠的食物摄入、体重和呼吸交换比 (RER)。

LH-21 是一种有效的体内中性大麻素 CB1受体拮抗剂。LH-21 会导致剂量依赖性进食抑制，减少肥胖 Zucker 大鼠的食物摄入和体重增加。

AM6545 是一种具有选择性和高效性的外周限制性大麻素受体 1 （CB1）拮抗剂，抑制 CB2 受体，可改善低代谢性肥胖并改善谷氨酸钠诱导的肥胖小鼠的脂肪因子分泌，可用于研究肥胖症和糖尿病。

GW438014A 是一种有效且具有选择性的 NPY-Y5 受体拮抗剂。GW438014A 对食物摄入并减少肥胖啮齿动物的体重增加具有抑制作用。

Naringenin chalcone (Isosalipurpol) 是一种黄酮醇生物合成的中间体，在查耳酮异构酶的作用下，自发代谢成柚皮素。它具有抗炎和抗过敏活性。

YM-440 is a novel hypoglycemic agent, an insulin sensitizer, that may be used for the treatment of type 2 diabetes mellitus by reducing glucose 6-phosphatase activity in obese Zucker rats and inhibiting liver glucose output through gluconeogenesis.

1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fasting alter hepatic lipid droplet proteome and diacylglycerol species and prevent diabetes in NZO mice. Biochim. Biophys. Acta 1851(5), 566-576 (2015).2. Narváez-Rivas, M., Vicario, I.M., Constante, E.G., et al. Changes in the concentrations of free fatty acid, monoacylglycerol, and diacylglycerol in the subcutaneous fat of Iberian ham during the dry-curing process. J. Agric. Food Chem. 55(26), 10953-10961 (2007). 1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2 References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fasting alter hepatic lipid droplet proteome and diacylglycerol species and prevent diabetes in NZO mice. Biochim. Biophys. Acta 1851(5), 566-576 (2015).2. Narváez-Rivas, M., Vicario, I.M., Constante, E.G., et al. Changes in the concentrations of free fatty acid, monoacylglycerol, and diacylglycerol in the subcutaneous fat of Iberian ham during the dry-curing process. J. Agric. Food Chem. 55(26), 10953-10961 (2007).

YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks.References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019). YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks. References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019).