Gemcabene (Synonyms: PD-72953) |
カタログ番号GC36128 |
クラス初の脂質低下剤であるゲムカベン (PD-72953) は、低密度リポタンパク質コレステロール (LDL-C) を低下させ、トリグリセリドを減少させ、高密度リポタンパク質コレステロール (HDL-C) を上昇させ、炎症誘発性を低下させます。抗炎症活性を発揮する急性期タンパク質、C反応性タンパク質(CRP)。
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Cas No.: 183293-82-5
Sample solution is provided at 25 µL, 10mM.
Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity[1][2][3].
Gemcabene calcium (PD-72953 calcium) significantly downregulates hepatic mRNA markers of inflammation (TNF-α, MCP-1, MIP-1β, CCR5, CCR2, NF-κB), lipogenesis and lipid modulation (ApoC-III, ACC1, ADH-4, Sulf-2), and fibrosis (TIMP-1 and MMP-2)[3].
[1]. Mandema JW, et al. Model-based development of gemcabene, a new lipid-altering agent. AAPS J. 2005 Oct 7;7(3):E513-22. [2]. Srivastava RAK, et al. Gemcabene, a First-in-Class Hypolipidemic Small Molecule in Clinical Development, Attenuates Osteoarthritis and Pain in Animal Models of Arthritis and Pain. Front Pharmacol. 2018 May 11;9:471. [3]. Oniciu DC, et al. Gemcabene downregulates inflammatory, lipid-altering and cell-signaling genes in the STAM™ model of NASH. PLoS One. 2018 May 30;13(5):e0194568.
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