产品
编 号:F086731
分子式:C17H29NO4
分子量:311.42
产品类型
结构图
CAS No: 1239600-18-0
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产品详情
生物活性:
LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.
体内研究:
LMT-28 (0-0.5 mg/kg;口服每天一次,持续 15 天) 减轻小鼠的 CIA。 LMT-28 (0.25 或 1 mg/kg;po) 改善小鼠胰腺炎的进展。LMT-28 直接特异性结合 gp130,从而抑制 gp130 与 IL-6/IL-6Rα 复合物的相互作用。Animal Model:Six-week-old male DBA/1J mice (collagen-induced arthritis mice, CIA)
Dosage:0-0.5 mg/kg
Administration:Oral; once daily for 15 days
Result:Markedly reduced the serum levels of cartilage oligomeric matrix protein (COMP) by 50%, serum amyloid P (SAP) by 55%, and anti-CII IgG by 62%.
体外研究:
LMT-28 在浓度为 50 μM 时可将 IL-6 诱导的荧光素酶活性降低约 90%,IC50 值为 5.9 μM。LMT-28 (1-10 μM;72 小时) 抑制 IL-6 诱导的人红白血病细胞系 TF-1 增殖。 LMT-28 (1-100 μM;1 小时) 选择性抑制 IL-6 诱导的 STAT3、JAK2 和 gp130 磷酸化。