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TG8-260作为一种新一代EP2拮抗剂,主要用于减缓炎症驱动的中枢神经系统及外周疾病的病理效应。研究表明,TG8-260可以显著降低匹罗卡品诱发的大鼠持续癫痫状态后海马区的神经炎症及胶质增生。此外,其药代动力学特性表明,TG8-260的血浆半衰期达2.14小时,口服生物利用度为77.3%。TG8-260亦为CYP450的有效抑制剂,能在BV2-hEP2小胶质细胞中抑制EP2受体介导的炎症基因表达,显示出其在外周炎症疾病动物模型中研究抗炎通路的潜在应用价值。
TG8-260作为一种新一代EP2拮抗剂,主要用于减缓炎症驱动的中枢神经系统及外周疾病的病理效应。研究表明,TG8-260可以显著降低匹罗卡品诱发的大鼠持续癫痫状态后海马区的神经炎症及胶质增生。此外,其药代动力学特性表明,TG8-260的血浆半衰期达2.14小时,口服生物利用度为77.3%。TG8-260亦为CYP450的有效抑制剂,能在BV2-hEP2小胶质细胞中抑制EP2受体介导的炎症基因表达,显示出其在外周炎症疾病动物模型中研究抗炎通路的潜在应用价值。
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 | TG8-260 is a second-generation EP2 antagonist developed to mitigate pathology in inflammatory-driven central and peripheral nervous system disorders. In a rat model, TG8-260 reduced neuroinflammation and gliosis in the hippocampal region following pilocarpine-induced status epilepticus. Pharmacokinetic data for TG8-260 reveal a plasma half-life of 2.14 hours and an oral bioavailability of 77.3%. Furthermore, TG8-260 acts as a potent inhibitor of CYP450 and demonstrates antagonistic activity by inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglial cells, making it suitable for research on anti-inflammatory pathways in animal models of peripheral inflammatory diseases. |
分子量 | 344.41 |
分子式 | C21H20N4O |
CAS No. | 2490544-50-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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