pparδ agonist 1

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

PPAR agonist 1 is an agonist of PPAR α/γ, used for reducing blood glucose, lipid levels, reducing body weight, and lowering cholesterol.

PPARα/δ agonist 1 是一种有效的 PPARα/PPARδ 双重激动剂，对 PPARα和 PPARδ 的 EC50 值分别为 7.0 nM 和 8.4 nM。PPARα/δ agonist 1 对 PPARγ 表现出很高的选择性 (EC50: 1316.1 nM)。PPARα/δ agonist 1 具有潜力进行非酒精性脂肪性肝炎的研究。

PPARα/γ agonist 1 是一种有效的双重 PPARα/γ部分激动剂，是用于研究血脂异常和糖尿病的有前途的化合物。PPARα/γ agonist 1 对 PPARα 和 PPARγ 的EC50值分别为 28 nM 和 69 nM。

PPARα agonist 1 是一种完整的、有效的 PPARα激动剂。

PPARγ agonist 1 是 PPARγ 的有效激动剂，能够高效的激活 hPPARγ ，并不引起完全激动，进而能够避免不良反应。PPARγ agonist 1 对代谢紊乱相关心血管疾病表现出研究潜力。

PPARδ agonist 11（Compound 11）作为一种具有选择性的PPARδ激动剂，其EC50值为20 nM。此化合物能有效降低LPS刺激下RAW264.7细胞产生的一氧化氮(NO)、TNFα和IL-6等促炎细胞因子，展现其通过NF-κB通路的抗炎活性。在人肝微粒体和血浆中，PPARδ agonist 11展现出优异的稳定性。此外，该化合物能显著改善Carrageenan引起的足部水肿，其药代动力学表现良好，生物利用度高达100％。

PPARδ agonist10 (compound 7) 是一种口服活性、选择性的PPARδ部分激动剂，对hPPARδ(LBD)-GAL4和mPPARδ的EC50值分别为0.053 μM和0.30 µM。在反式激活测定中，PPARδ agonist10 作为部分PPARδ激动剂，但在体外和体内均能完全激活肌肉细胞的游离脂肪酸氧化。该化合物适用于血脂异常的研究。

PPARγ agonist10 (compound 33g) 作为一种PPARγ激动剂，能有效促进βTC6细胞的胰岛素分泌、葡萄糖摄取以及提高胰岛素敏感性。

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)

CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Chem.63(15)8369-8379(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。

PPARδ agonist9 (compound 21) 作为PPARδ激动剂，展现出EC50为3.6 nM的活性。在体内实验中，PPARδ agonist9能有效降低小鼠血清中MCP-1水平，并在LDLr-KO模型中显著抑制动脉粥样硬化的发展，其抑制率达50-60%。