1239600-18-0
基本信息
LMT-28 >=98% (HPLC)
2-Oxazolidinone, 3-[(2S,3S)-3-hydroxy-2-methyl-4-methylene-1-oxononyl]-4-(1-methylethyl)-, (4S)-
常見問題列表
IL-6
|
LMT-28 reduces IL-6-induced luciferase activity by ~90% at a concentration of 50 μM and exhibits an IC
50
value of 5.9 μM. LMT-28 (1-10 μM; 72 hours) inhibits IL-6-induced proliferation of the human erythroleukemic cell line TF-1.
LMT-28 (1-100 μM; 1 hour) selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.
Cell Proliferation Assay
Cell Line: | TF-1 cells (1 ng/mL IL-6-induced) |
Concentration: | 1, 10, 100, 1000, 10000 nM |
Incubation Time: | 72 hours |
Result: | Markedly inhibited IL-6–induced TF-1 proliferation with an IC50 value of 7.5 μM. |
Western Blot Analysis
Cell Line: | HepG2 cells (treated with 10 ng/mL IL-6) |
Concentration: | 1, 3, 10, 30, and 100 μM |
Incubation Time: | 1 hour |
Result: | Inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130. |
LMT-28 (0-0.5 mg/kg; p.o.; once daily for 15 days) alleviates CIA in mice.
LMT-28 (0.25 or 1 mg/kg; p.o.) ameliorates the progression of pancreatitis in mice. LMT-28 binds directly and specifically to gp130, and thereby inhibits the interaction of gp130 with the IL-6/IL-6Rα complex.
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%. |