ob/ob

OB 24 hydrochloride is a potent and selective heme oxygenase 1 (HO-1) inhibitor (IC50 values are 1.9 and >100 μM for HO-1 and HO-2 respectively), reduces protein carbonylation and reactive oxygen species formation in advanced prostate cancer cells (PCA). Inhibits cell proliferationin vitroand PCA tumor growth and lymph node/lung metastasesin vivo. Synergizes with Taxol.

OB-1 是一种口蛋白样蛋白-3 (STOML3) 抑制剂，通过下调 PPARγ通路抑制成脂分化和 LD 生长。OB-1 通过干扰气孔素的自缔合，抑制脂肪生成并阻碍脂滴生长。

OB-2 is an inhibitor of stomatin-like protein-3 (STOML3) oligomerization. OB-2 reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in vivo.

OB-24 free base is a potent and selective heme oxygenase 1 (HO-1) inhibitor.

[D-Leu-4]-OB3 抑制促炎、增殖和转移基因的表达以及 PD-L1的表达。[D-Leu-4]-OB3 刺激促凋亡基因的表达。

OB3, 相比于Leptin，在降低小鼠模型的肥胖和糖尿病方面显示出更高效。此化合物能够降低肝癌细胞内瘦素相关的炎症及其增殖作用。

Fatostatin hydrobromide (Fatostatin A HBr) 是一种 SREBP 活化的特异性抑制剂，可抑制 SREBP-1 和 SREBP-2 的活化。它与 SCAP (SREBP 裂解激活蛋白) 结合，抑制 SREBPs 的 ER-Golgi 易位。它具有抗肿瘤作用，能抑制 ob/ob 小鼠的高血糖。它抑制了细胞中成脂基因的转录。

Fatostatin A 是一种SREBP 活化的特异性抑制剂，能够抑制 SREBP-1 和 SREBP-2 的活化。它与 SCAP (SREBP 裂解激活蛋白) 结合，抑制 SREBPs 的 ER-Golgi 易位。它具有抗肿瘤活性，能抑制ob/ob 小鼠的高血糖。它抑制细胞中成脂基因的转录。

Talibegron hydrochloride (ZD2079 hydrochloride) 是一种β3肾上腺素能受体激动剂，对苯肾上腺素预收缩大鼠肠系膜动脉的 pD2为3.72。松弛大鼠肠系膜动脉和离体主动脉。在体内抑制瘦小鼠 ob 基因表达和循环瘦素水平。

MK-0812 是一种 CCR2 受体和 CCR5 受体双重拮抗剂，可减轻 ob/ob 小鼠的脂肪炎症。

PF-5006739 is an effective and selective inhibitor of CK1δ ε (IC50s: 3.9 nM and 17.0 nM, respectively). PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ ε and high kinome selecti

DDN 是一种选择性胰岛素受体 (Insulin Receptor) 激活剂和胰岛素增敏剂，同时也是具有降血糖活性的胰岛素模拟物，具备口服有效性。其能够直接结合受体激酶结构域，诱导Akt与ERK磷酸化，并增强胰岛素对葡萄糖吸收的刺激作用。DDN 明显降低野生型及糖尿病 ob ob 和 db db 小鼠的血糖水平。

AM-2394 是新型的 glucokinase 激活剂 (GKA)。它能够激活葡萄糖激酶 (GK)，EC50=60 nM。

BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, in association with increased intact form of hFGF21 in ob ob mice. BR103354 acts as an effective FAP inhibitor in vitro and in vivo, thereby demonstrating its potential application as an anti-diabetic and anti-NASH agent.

INU-101 is an 11β-HSD1 inhibitor. In KKAy mice, ob ob mice, and ZDF rats, oral administration of INU-101 led to enhanced insulin sensitivity and the lowering of the fasting level of glucose in the blood. INU-101 therefore shows promise as a potential treatment for type 2 diabetes and metabolic syndrome.

BMS-763534 is a potent antagonist of corticotropin-releasing factor hormone receptor 1 (CRHR-1).

4-Aaqb, also known as OB-318, is a natural inhibitor of the autophagy pathway, enhancing immune function, suppressing MAPK and NFκB, showing anti-inflammatory, hypoglycemic, vasorelaxative, and antiproliferative activities.

胃抑制肽1(GIP-1) (3-42)是肠促胰岛素激素GIP的一个肽段，同时也是GIP受体的拮抗剂。它通过血清二肽基肽酶4(DDP-4)从GIP中形成。GIP-1 (3-42) (100 nM)在减少BRIN-BD11胰腺细胞的胰岛素分泌方面起作用。在以25 nmol/kg剂量给药的ob/ob糖尿病小鼠模型中，它能增加血浆葡萄糖水平并降低血浆胰岛素水平。

ZG-2291是一种有口服活性的FIH(缺氧诱导因子抑制剂)选择性抑制剂.它通过与FIH结合并引发关键酪氨酸的构象变化,实现对FIH的特异性抑制,同时不干扰其他JmjC家族的2OG氧化酶.此外,ZG-2291还能增强ob ob小鼠的产热功能,改善肥胖症及代谢功能障碍,显示出在治疗肥胖病领域的研究潜力.

Leptin(22-56),human is a peptide fragment of Leptin, which ACTS through a variety of subtypes of Ob-Rs.

GIP receptor antagonist (IC50 = 2.6μM). Inhibits GIP-stimulated insulin release from pancreatic β cells in vitro. In ob/ob mice, blocks the effects of GIP on insulin release and plasma glucose levels. Also improves intraperitoneal glucose tolerance, insul