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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 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%。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | Compound 11, a selective PPARδ agonist, demonstrates an EC50 of 20 nM, indicating its high affinity for PPARδ receptors. This compound efficiently reduces levels of nitric oxide (NO), as well as the pro-inflammatory cytokines TNFα and IL-6 in LPS-stimulated RAW264.7 cells via the NF-κB pathway, showcasing its anti-inflammatory properties. Additionally, Compound 11 exhibits remarkable stability in human liver microsomes and plasma. It significantly ameliorates foot edema induced by Carrageenan, displaying favorable pharmacokinetic properties with a bioavailability of approximately 100%. |
靶点活性 | PPARδ (human):0.02 μM (EC50), PPARα (human):8 μM (EC50) |
分子量 | 440.46 |
分子式 | C19H15F3N2O3S2 |
CAS No. | 2982696-04-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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