LMT-28

LMT-28

中文名称LMT-28
中文同义词(4S)-3-[(2S,3S)-3-羟基-2-甲基-4-亚甲基-1-氧代癸烷基]-4-(1-甲基乙基)-2-恶唑烷酮;化合物 T15769;化合物LMT-28
英文名称LMT-28
英文同义词LMT-28;2-Oxazolidinone, 3-[(2S,3S)-3-hydroxy-2-methyl-4-methylene-1-oxononyl]-4-(1-methylethyl)-, (4S)-;LMT-28 >=98% (HPLC);LMT28,LMT 28
CAS号1239600-18-0
分子式C17H29NO4
分子量311.42
EINECS号
相关类别
Mol文件1239600-18-0.mol
结构式LMT-28 结构式

LMT-28 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 的 DMSO (321.11 mM) 溶液,
酸度系数(pKa)13.97±0.20(Predicted)
形态油状
颜色无色至淡黄色
水溶解性< 0.1 mg/mL Water (insoluble)

LMT-28 用途与合成方法

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。

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%.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-102084LMT-281 mg320元
2024/04/30HY-102084LMT-28
LMT-28
1239600-18-05mg800元

LMT-28 上下游产品信息

"LMT-28"相关产品信息
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