ppar-δ

GW 7647 是一种有效且高度选择性的 PPAR α 激动剂，人 PPAR α、PPAR γ 和 PPAR δ 受体的 EC 50 值分别为 6、1100 和 6200 nM ）。GW 7647 能减少巨噬细胞中一氧化氮的产生，在体内有降脂和抗炎特性。

Seladelpar (MBX 8025) 是一种有效的，具有口服活性的， 特异性PPAR-δ激动剂，EC50为 2 nM。

Indeglitazar (PPM 204) 是 PPAR 的泛激动剂，包括亚型 alpha (α)、delta (δ) 和 gamma (γ)。

Bocidelpar 是一种有效的过氧化物酶体增殖物激活受体 delta 调节剂，可改善杜兴肌营养不良肌肉细胞中的线粒体生物合成和功能。

Elafibranor (GFT505) 是过氧化物酶体增殖物激活受体-α (PPAR-α) 和过氧化物酶体增殖物激活受体-δ (PPAR-δ) 的激动剂，EC50 值分别为 45 和 175 nM。

Imiglitazar (TAK559)是有效的 PPAR-β δ受体激动剂，具有降血糖作用。

Seladelpar lysine, a selective PPAR-δ agonist, is used for the therapy of Homozygous Familial Hypercholesterolemia (HoFH).

The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively. CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM).

Anti-NASH agent 1 (compound 3d)，Elafibranor衍生物，高效PPAR-α/δ激动剂，针对非酒精性脂肪性肝炎（NASH）。以3-10 mg/kg剂量，连续4周处理，能显著改善蛋氨酸胆碱缺乏（MCD）诱导的NASH小鼠高脂血症、肝脏脂肪变性及炎症状况，展现出低肝毒性和良好肝脏保护效能。

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

Pparδ agonist 1 is an agonist of PPAR-δ(EC50 of 5.06 nM).

PT-S58 is a PPAR β/δ full antagonist, and a derivative of GSK0660. PT-S58 has a three-fold higher affinity for the receptor than GSK0660 and is a potent inhibitor of agonist-induced target gene expression. PT-S58 are effective on PPRE-independent functions of PPARβ/δ. Unlike GSK0660, PT-S58 blocks the recruitment co-repressor molecules such as SMRT.