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编 号：F199141
分子式：C18H19FN6
分子量：338.38
分子式：C18H19FN6
分子量：338.38
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CAS No: 165806-53-1
产品详情
生物活性：
SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
体内研究：
SB 220025 (3-50 mg/kg; p.o.; single) 可抑制体内炎症细胞因子的产生。SB 220025 (5, 30, 50 mg/kg; i.p.; bid) 抑制小鼠气囊肉芽肿模型的血管生成。SB 220025 (30 mg/kg; p.o.; twice a day for 3, 5, 7 or 14 days) 防止小鼠气囊血管生成模型第 3 天后发生的血管生成增加。SB 220025 (50 mg/kg; p.o.; b.i.d.; 10 days) 在慢性炎症疾病模型中有效地阻止关节炎的进展。Animal Model:Acute model of LPS-induced TNF-a expression.
Dosage:3-50 mg/kg
Administration:Oral administration; single; 30 min before challenge with LPS.
Result:Dosedependently inhibited TNF-a production with an ED50 value of 7.5 mg/kg, and showed more than 80% inhibition when at 50 mg/kg.
Animal Model:Murine air pouch granuloma model.
Dosage:5, 30, 50 mg/kg
Administration:Intraperitoneal injection; bisindie (bid, twice a day).
Result:Caused a dose-dependent reduction in angiogenesis.
Animal Model:Murine air pouch granuloma model.
Dosage:30 mg/kg
Administration:Oral administration; twice a day from day 0 until removal of granuloma tissue at days 3, 5, 7 or 14.
Result:Did not affect the initial burst of angiogenesis but did prevent the increase in angiogenesis that occurs after day 3.
体外研究：
SB 220025 (20 μM; 6 h) 显着降低 HUVEC 细胞中响应球型脂联素 (gAd) 的 IL-8 基因表达。
SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
体内研究：
SB 220025 (3-50 mg/kg; p.o.; single) 可抑制体内炎症细胞因子的产生。SB 220025 (5, 30, 50 mg/kg; i.p.; bid) 抑制小鼠气囊肉芽肿模型的血管生成。SB 220025 (30 mg/kg; p.o.; twice a day for 3, 5, 7 or 14 days) 防止小鼠气囊血管生成模型第 3 天后发生的血管生成增加。SB 220025 (50 mg/kg; p.o.; b.i.d.; 10 days) 在慢性炎症疾病模型中有效地阻止关节炎的进展。Animal Model:Acute model of LPS-induced TNF-a expression.
Dosage:3-50 mg/kg
Administration:Oral administration; single; 30 min before challenge with LPS.
Result:Dosedependently inhibited TNF-a production with an ED50 value of 7.5 mg/kg, and showed more than 80% inhibition when at 50 mg/kg.
Animal Model:Murine air pouch granuloma model.
Dosage:5, 30, 50 mg/kg
Administration:Intraperitoneal injection; bisindie (bid, twice a day).
Result:Caused a dose-dependent reduction in angiogenesis.
Animal Model:Murine air pouch granuloma model.
Dosage:30 mg/kg
Administration:Oral administration; twice a day from day 0 until removal of granuloma tissue at days 3, 5, 7 or 14.
Result:Did not affect the initial burst of angiogenesis but did prevent the increase in angiogenesis that occurs after day 3.
体外研究：
SB 220025 (20 μM; 6 h) 显着降低 HUVEC 细胞中响应球型脂联素 (gAd) 的 IL-8 基因表达。
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