产品
编 号:F405944
分子式:C11H16FN3O3
分子量:257.26
产品类型
结构图
CAS No: 61422-45-5
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产品详情
生物活性:
Carmofur (HCFU) is a rat recombinant acid ceramidase inhibitor with an IC50 of 29 nM. Carmofur is also a protease inhibitor of SARS-CoV-2 main protease (Mpro), fatty acid amide hydrolase (FAAH) and N-acylethanolamine acid amidase (NAAA). Carmofur has anti-cancer, anti-inflammatory and anti-virus activities, and can be used for the study of COVID-19 and acute lung injury (ALI).
体内研究:
Carmofur (10-30 mg/kg; 腹腔注射,单剂量) 在雄性瑞士韦伯斯特小鼠中抑制各个组织的 (包括肺和脑皮层) 的酸性神经酰胺酶 (AC) 活性。Carmofur (10 mg/kg; 口服, 单剂量) 在急性肺损伤 (ALI) C57BL/6J 小鼠中通过抑制 FAAH 和 NAAA 的活性来显著改善脂多糖 (LPS) (5 mg/kg; 气管灌注,单剂量) (HY-D1056) 诱导的炎症反应,促进肺损伤的消退。Animal Model:Male C57BL/6J mice model of LPS-induced ALI
Dosage:3 mg/kg, 10 mg/kg
Administration:Oral gavage (p.o.), single dose. After LPS treatment (5 mg/kg; Tracheal perfusion, single dose)
Result:Significantly inhibited MPO activity, which is a marker of neutrophil abundance.Alleviated alveolar edema and inhibited neutrophil accumulation.
体外研究:
Carmofur (0.3-10 μM; 20 min-1 h) 在人结肠癌 SW403 细胞中以浓度和时间依赖方式降低酸性神经酰胺酶 (AC) 的活性。Carmofur (1-100 μM; ) 在 Vero E6 细胞中抑制 SARS-CoV-2 的活性 EC50 为 24.3 μM。Carmofur (5 μM; 6 h) 在 HEK293 细胞中能抑制 FAAH 和 NAAH 的活性,IC50 为0.11 μM 和 0.71 μM。Carmofur (10 μM; 30 min) 在 Raw264.7 细胞中具有抗炎活性。