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CAS No. : 188791-09-5
MCE 国际站:JTE-607
产品活性:JTE-607 是一种高选择性的炎性细胞因子合成抑制剂,可保护小鼠免受内毒素休克。JTE-607 作用于 LPS 刺激的人 PBMC,抑制 TNF-α、IL-1β、IL-6、IL-8 和 IL-10 的 IC50 分别为 11、5.9、8.8、7.3 和 9.1 nM。断裂和聚腺苷酸化特异因子 3 (CPSF3) 是 JTE-607的靶蛋白。
研究领域:Immunology/Inflammation
作用靶点:Interleukin Related
In Vitro: JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. The inhibitory effects of JTE-607 are also seen in mRNA expression of those cytokines.
JTE-607 inhibits inflammatory cytokine production from LPS-stimulated human PBMCs with an IC50 of approximately 10 nM.
JTE607 inhibits LPS-stimulated IL-8 production from monkey and rabbit PBMCs, and TNF-α production from mouse and rat PBMCs with IC50s of 59, 780, 1600 and 19000 nM, respectively.
JTE607 also suppresses other cytokines, granulocyte-macrophage colony stimulating factor and IL-1RA with IC50s of 2.4±0.8 and 5.4±0.4 nM, respectively.
JTE-607 inhibits cytokine production in monkey, rabbit, mouse and rat with IC50s of 59±26, 780±120, 1600±650 and 19000±3200 nM, respectively.
In Vivo: JTE-607 (0.3-10 mg/kg, i.v.) shows dose dependent inhibition of mortality after LPS challenge in C. parvum sensitized mice in accordance with a decrease of plasma TNF-α.
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