产品
编 号:F756196
分子式:C21H17ClN6OS
分子量:436.92
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1mg
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5mg
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10mg
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25mg
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生物活性:
Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 μM, >5 μM, >5 μM, >5 μM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity.

体内研究:
Cathepsin C-IN-5 (1500 mg/kg) 在 ICR 小鼠中给药后 7 天内未显示明显的体重减轻或毒性反应。 Cathepsin C-IN-5 (口服 10 mg/kg;静脉注射 2 mg/kg) 显示出良好的生物利用度,F=42.07%。 Cathepsin C-IN-5 (2,10,50 mg/kg;po) 在 ALI 动物模型中显示出有效的抗炎活性和潜在的保护作用。Animal Model:C57BL/6 male mice (acute lung injury (ALI) mice model)
Dosage:2, 10, 50 mg/kg (one hour after administration, received LPS (20 mg/kg))
Administration:P.o.
Result:Decreased the levels of proinflammatory cytokines (TNF-a, IL-6, and GM-CSF) and increased the the concentration of the anti-inflammatory cytokine (IL-10) in a dose-dependent manner.

体外研究:
Cathepsin C-IN-5 (化合物 SF38) 在 THP-1 和 U937 细胞中表现出抑制作用,IC50 分别为 115.4、70.2 nM。
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