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编 号:F741124
分子式:C44H60IN5O4
分子量:849.88
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生物活性:
EM-163 is a summative BB-Loop analog. EM-163 can alleviate inflammation and prevent death from toxic shock by targeting the TIR domain of MyD88. EM-163 can be used in the study of SEB poisoning (SEB: Staphylococcal enterotoxin B).

体内研究:
EM-163 (0.21-0.86 mg/mouse; 腹腔注射; 单剂量) 能够有效抑制促炎细胞因子的释放,延迟或避免葡萄球菌肠毒素 B (SEB) 对 BALB/c 小鼠引起的中毒性休克导致的死亡。Animal Model:SEB-induced BALB/c mice model
Dosage:0.21 mg/mouse, 0.42 mg/mouse, 0.86 mg/mouse
Administration:Intraperitoneal injection (i.p.); Single dose. Before SEB treatment (0.5 μg/mouse, 5 μg/mouse; i.p.; single dose) and LPS treatment.
Result:Delayed mouse death at a dose of 0.21 mg/mouse, and protected mice from death at either dose of 0.42 mg/mouse or 0.86 mg/mouse.Delayed mouse death even at high doses of SEB (5 μg).

体外研究:
EM-163 (50-100 μg/mL) 可以靶向 TIR 结构域,能与 TIR 结构域的蛋白结合且可以抑制 TIR-TIR 结构域的相互作用。EM-163 (10-500 μM; 30 min) 在人类单核细胞 (MNS) 中抑制了 SEB (200 ng/mL) 诱导的 TNF-α、IFN-γ、IL-2 和 IL-1b 的产生。
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