产品
编 号：F369247
分子式：C25H22N4O4
分子量：442.47
分子式：C25H22N4O4
分子量：442.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
195
In-stock
5mg
390
In-stock
10mg
624
In-stock
50mg
1880
In-stock
100mg
2240
In-stock
结构图
CAS No: 496775-61-2
产品详情
生物活性：
Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well.
体内研究：
Eltrombopag Olamine (10 mg/kg；每天口服一次，持续 5 天) 在黑猩猩中表现出良好的耐受性。Eltrombopag Olamine (17.6 mg/kg；腹腔注射；每天一次，持续 2 天) 显著降低平均金黄色葡萄球菌在小鼠鼻腔感染中的计数。Animal Model:Female chimpanzees
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once a day; for 5 days
Result:Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.
Animal Model:C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 108 CFU suspended in 40 μL PBS) into the nasal cavities)
Dosage:17.6 mg/kg
Administration:IP; once a day for 2 days
Result:Significantly reduced mean bacterial counts (5.0 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) mice.
体外研究：
Eltrombopag (0.002-50 μM；4 h) 在转染荧光素酶报告基因的小鼠 BAF3 细胞中具有活性。 Eltrombopag (30 μM；120 min) 影响 p 的激活-N2C-Tpo 细胞中的 STAT5。 Eltrombopag (30 μM；120 分钟) 激活巨核细胞中的 p-STAT5。 Eltrombopag (0.1 nM-10 μM；30 min) 刺激 BAF3/hTpoR 细胞增殖。 Eltrombopag (0.03-3 μM；10 days) 增加骨髓分化CD34+ 细胞转变为 CD41+ 巨核细胞。 Eltrombopag (0-3 μM；72 h) 影响 N2C-Tpo细胞凋亡。 Eltrombopag 有效抑制肺炎球菌生长，MIC50 为 0.3 mg/L，但对革兰氏阴性菌。 Eltrombopag (0 -200 mg/L；24 小时；Caco-2 和 HepG2 细胞) 抑制金黄色葡萄球菌的生长 MIC50 为 1.5 mg/L，与 Vancomycin 共同处理时表现出更高的效力，MIC50 为 1.2 mg/L。 Eltrombopag (0 或 10 μg/mL；72 h) 显著诱导 Huh7 细胞的 G0/G1 期阻滞。 Eltrombopag (0.1-100 μg/mL；72 h) 对 HCC 细胞系具有抗增殖活性。
Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well.
体内研究：
Eltrombopag Olamine (10 mg/kg；每天口服一次，持续 5 天) 在黑猩猩中表现出良好的耐受性。Eltrombopag Olamine (17.6 mg/kg；腹腔注射；每天一次，持续 2 天) 显著降低平均金黄色葡萄球菌在小鼠鼻腔感染中的计数。Animal Model:Female chimpanzees
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once a day; for 5 days
Result:Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.
Animal Model:C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 108 CFU suspended in 40 μL PBS) into the nasal cavities)
Dosage:17.6 mg/kg
Administration:IP; once a day for 2 days
Result:Significantly reduced mean bacterial counts (5.0 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) mice.
体外研究：
Eltrombopag (0.002-50 μM；4 h) 在转染荧光素酶报告基因的小鼠 BAF3 细胞中具有活性。 Eltrombopag (30 μM；120 min) 影响 p 的激活-N2C-Tpo 细胞中的 STAT5。 Eltrombopag (30 μM；120 分钟) 激活巨核细胞中的 p-STAT5。 Eltrombopag (0.1 nM-10 μM；30 min) 刺激 BAF3/hTpoR 细胞增殖。 Eltrombopag (0.03-3 μM；10 days) 增加骨髓分化CD34+ 细胞转变为 CD41+ 巨核细胞。 Eltrombopag (0-3 μM；72 h) 影响 N2C-Tpo细胞凋亡。 Eltrombopag 有效抑制肺炎球菌生长，MIC50 为 0.3 mg/L，但对革兰氏阴性菌。 Eltrombopag (0 -200 mg/L；24 小时；Caco-2 和 HepG2 细胞) 抑制金黄色葡萄球菌的生长 MIC50 为 1.5 mg/L，与 Vancomycin 共同处理时表现出更高的效力，MIC50 为 1.2 mg/L。 Eltrombopag (0 或 10 μg/mL；72 h) 显著诱导 Huh7 细胞的 G0/G1 期阻滞。 Eltrombopag (0.1-100 μg/mL；72 h) 对 HCC 细胞系具有抗增殖活性。
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