LMT-28
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- CAS号:
- 1239600-18-0
- 英文名:
- LMT-28
- 英文别名:
- LMT-28;LMT28,LMT 28;LMT-28 >=98% (HPLC);2-Oxazolidinone, 3-[(2S,3S)-3-hydroxy-2-methyl-4-methylene-1-oxononyl]-4-(1-methylethyl)-, (4S)-
- 中文名:
- LMT-28
- 中文别名:
- 化合物LMT-28;化合物 T15769;(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
- CBNumber:
- CB54670121
- 分子式:
- C17H29NO4
- 分子量:
- 311.42
- MOL File:
- 1239600-18-0.mol
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LMT-28化学性质
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沸点:
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452.9±38.0 °C(Predicted)
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密度:
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1.065±0.06 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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100 mg/mL in DMSO (321.11 mM),
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酸度系数(pKa):
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13.97±0.20(Predicted)
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形态:
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oil
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颜色:
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colorless to light yellow, oil
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水溶解性:
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< 0.1 mg/mL Water (insoluble)
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LMT-28性质、用途与生产工艺
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。
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
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Cell Line:
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TF-1 cells (1 ng/mL IL-6-induced)
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Concentration:
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1, 10, 100, 1000, 10000 nM
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Incubation Time:
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72 hours
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Result:
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Markedly inhibited IL-6–induced TF-1 proliferation with an IC50 value of 7.5 μM.
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Western Blot Analysis
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Cell Line:
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HepG2 cells (treated with 10 ng/mL IL-6)
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Concentration:
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1, 3, 10, 30, and 100 μM
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Incubation Time:
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1 hour
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Result:
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Inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.
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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.
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Animal Model:
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Six-week-old male DBA/1J mice (collagen-induced arthritis mice, CIA)
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Dosage:
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0-0.5 mg/kg
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Administration:
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Oral; once daily for 15 days
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Result:
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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%.
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LMT-28
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-102084 | LMT-28 | | 1 mg | 320元 |
| 2024/04/30 | HY-102084 | LMT-28
LMT-28 | 1239600-18-0 | 5mg | 800元 |
1239600-18-0, LMT-28 相关搜索:
- 化合物LMT-28
- 化合物 T15769
- (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
- 1239600-18-0
- LMT28,LMT 28
- LMT-28 >=98% (HPLC)
- 2-Oxazolidinone, 3-[(2S,3S)-3-hydroxy-2-methyl-4-methylene-1-oxononyl]-4-(1-methylethyl)-, (4S)-
- LMT-28