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Pirinixic acid

CAS No. : 50892-23-4

MCE 站：Pirinixic acid

产品活性：Pirinixic acid (Wy-14643) 是一种有效的 PPARα 激动剂，对鼠的 PPARα 和 PPARγ 的 EC₅₀ 值分别为 0.63 μM, 32 μM，对人的 PPARα，PPARγ 和 PPARδ 的 EC₅₀ 值分别为 5.0 μM，60 μM，35 μM。

研究领域：Cell Cycle/DNA Damage

作用靶点：PPAR

In Vitro: Pirinixic acid (Wy-14643) is an agonist of PPARα, with EC₅₀s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively. Pirinixic acid (Wy-14643; 0, 10, 100 μM) enhances protein expression of PPAR-α in synovial fibroblasts. Pirinixic acid (0, 10, 100 μM) shows inhibitroy effects on NO and PGE2 production in LPS-stimulated synovial fibroblasts. Pirinixic acid also effectively downregulates expression of inflammatory mediators such as VCAM-1, ICAM-1, ET-1, and TF in synovial fibroblasts, blocks LPS-induced NF-kB activation, IkB phosphorylation, and NF-kB nuclear translocation in synovial fibroblasts, but Pirinixic acid shows no effects in PPAR-α silenced cells.

In Vivo: Pirinixic acid (Wy-14643; 10?mg/kg, i.v.) decreases hepatic injury and lipid peroxidation (MDA) levels in obese rats. Pirinixic acid also causes increased SIRT1 activity in Sham and ischemia-reperfusion (IR) group, but shows no effects on SIRT3 protein expression. Pirinixic acid enhances NAD⁺, and ATP levels, and prevents endoplasmic reticulum stress (ERS) in rats.

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