pparδ agonist 2

Pparδ agonist 2 is an agonist of PPARδ.

PPARγ agonist 2 is a highly effective compound that acts as a partial agonist for PPARγ. It exhibits significant potential for utilization in metabolic disease research [1].

2-Bromohexadecanoic acid (2-BP) 是一种不可代谢的棕榈酸酯类似物，一种 PPARδ 的激动剂，可用作棕榈酰化抑制剂，抑制 DHHC 介导的棕榈酰化。

Seladelpar sodium salt (MBX-8025) 是一种具有口服活性、有效且特异性的PPARδ激动剂，EC50值为 2 nM。它对 PPARδ 的选择性分别是对 PPARα 和 PPARγ 的 750 和 2500 多倍。

E17241作为ABCA1基因表达的诱导剂，具有显著的生物活性（EC50 = 280 nM）。它同时也是一种过氧化物酶体增殖激活受体（PPARs）的激动剂，在HepG2细胞中能通过激活PPARγ、PPARα和PPARδ，促进PPAR介导的基因表达（EC50分别为290, 3,900, 和879 nM）。在RAW 264.7巨噬细胞中，E17241可以增强ABCA1蛋白的水平，这一作用在使用针对PKCζ mRNA的siRNA时失效。在用E17241处理的RAW 264.7细胞中，当浓度为0.4, 2, 或 10 µM时，可增加胆固醇的外流。此外，针对ApoE-/-小鼠的动脉粥样硬化模型表明，每日25 mg/kg的E17241剂量能有效降低血浆中的胆固醇、丙氨酸转氨酶（ALT）、天门冬氨酸转氨酶（AST）水平以及肝脏中的胆固醇和甘油三酯含量，且减少了主动脉的病变面积。此外，每日50 mg/kg的E17241剂量可以在高脂高糖（HFHG）饮食下减轻KKAy糖尿病小鼠的血糖水平和体重。

PPARγ/δ modulator 2 (Compound 3h) 是一种PPARγ的激动剂与PPARδ的拮抗剂，分别对PPARγ和PPARδ的Ki值为2.8 μM和43 nM。该化合物显著提高脂联素 (Adiponectin) 生成，并促进人骨髓间充质干细胞 (hBM-MSCs) 的脂肪分化，可用于研究与低脂联素血症相关的代谢性疾病。

15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester 是 15-Deoxy-Δ-12,14-prostaglandin J2 的衍生物。15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) 是一种环戊烯酮前列腺素，也是 PGD2 的代谢产物。它作为选择性的PPARγ激动剂（EC50为 2 µM）和共价的PPARδ激动剂，能够有效促进 C3H10T1/2 成纤维细胞向脂肪细胞的分化，其EC50为 7 μM。

MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transaminase (ALT), as well as serum and hepatic cholesterol and triglyceride, levels and reduces markers of NASH in the same model. |1. Bays, H.E., Schwartz, S., Littlejohn, T., 3rd, et al. MBX-8025, a novel peroxisome proliferator receptor-δ agonist: Lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin. J. Clin. Endocrinol. Metab. 96(9), 2889-2897 (2011).|2. Haczeyni, F., Wang, H., Barn, V., et al. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol. Commun. 1(7), 663-674 (2017).

ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. 1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020)

GW0742 是一种有效且特异性的 PPARδ 激动剂，对人 PPARδ、PPARα 和 PPARγ 的 EC50值分别为 1、1.1 和 2 μM。

TUG-1375 是游离脂肪酸受体 2 (FFA2/GPR43) 激动剂(pKi:6.69)。它对 FFA3，FFA4，PPARα，PPARγ，PPARδ，LXRα 或 LXRβ 无作用。