LMT-28

生物活性靶点体外研究体内研究 LMT-28 试剂级价格

LMT-28

CAS号:1239600-18-0
英文名:LMT-28
中文名:LMT-28
CBNumber:CB54670121
分子式:C17H29NO4
分子量:311.42
MOL File:1239600-18-0.mol

LMT-28化学性质

沸点 :452.9±38.0 °C(Predicted)
密度 :1.065±0.06 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :100 mg/mL in DMSO (321.11 mM),
酸度系数(pKa) :13.97±0.20(Predicted)
形态 :oil
颜色 :colorless to light yellow, oil
水溶解性 :< 0.1 mg/mL Water (insoluble)

LMT-28性质、用途与生产工艺

生物活性 LMT-28 是一种具有口服活性的通过直接与 gp130 结合而发挥作用的 IL-6 抑制剂。LMT-28 具有低毒性，并选择性抑制 IL-6 诱导的 STAT3、JAK2 和 gp130 的磷酸化。
靶点

IL-6

体外研究

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.

体内研究

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%.