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- Janus kinase (JAK)
- LMT-28
LMT-28
LMT-28 是一种具有口服活性的合成 IL-6 抑制剂，通过直接结合 gp130 发挥作用。
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包装价格促销价数量
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5mg￥875.00700.00- +
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10mg￥1525.001220.00- +
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25mg￥3262.002610.00- +
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50mg￥5400.004320.00- +
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100mg￥9175.007340.00- +
- 货号: ajcx11588
- CAS: 1239600-18-0
- 别名:
- 分子式: C??H??NO?
- 分子量: 311.42
- 纯度: ＞98%
- 溶解度: 100 mg/mL in DMSO (321.11 mM), < 0.1 mg/mL Water (insoluble)
- 储存: Store at -20°C
- 库存: 现货
Background
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[1].
LMT-28 reduces IL-6-induced luciferase activity by ~90% at a concentration of 50 μM and exhibits an IC50 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[1].
LMT-28 (1-100 μM; 1 hour) selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130[1].
LMT-28 (0-0.5 mg/kg; p.o.; once daily for 15 days) alleviates CIA in mice[1].
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[1].
Reference:
[1]. Hong SS, et al. A Novel Small-Molecule Inhibitor Targeting the IL-6 Receptor β Subunit, Glycoprotein 130. J Immunol. 2015 Jul 1;195(1):237-45.
