Eltrombopag

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^{[1][2][3][4][5]}. IC50 & Target: Thrombopoietin Receptor, Staphylococcus aureus, Apoptosis^[1][3][5] In Vitro: Eltrombopag (0.002-50 μM; 4 h) possesses activity in murine BAF3 cells transfected with the luciferase reporter gene^[1].
Eltrombopag (30 μM; 120 min) affects the activates of p-STAT5 in N2C-Tpo cells^[1].
Eltrombopag (30 μM; 120 min) activates p-STAT5 in megakaryocytes^[1].
Eltrombopag (0.1 nM-10 μM; 30 min) stimulates proliferation of BAF3/hTpoR cells^[1].
Eltrombopag (0.03-3 μM; 10 days) increases the differentiation of bone marrow CD34⁺ cells into CD41⁺ megakaryocytes^[1].
Eltrombopag (0-3 μM; 72 h) affects N2C-Tpo cell apoptosis^[1].
Eltrombopag efficiently inhibits Pneumococcal growth with MIC₅₀ of 0.3 mg/L, but shows no activity against Gram-negative bacteria^[3].
Eltrombopag (0-200 mg/L; 24 h; Caco-2 and HepG2 cells) inhibits Staphylococcus aureus growth with an MIC₅₀ of 1.5 mg/L, and exhibits higher potency when co-treats with Vancomycin (HY-B0671) with an MIC₅₀ of 1.2 mg/L^[3].
Eltrombopag (0 or 10 μg/mL; 72 h) significantly induces G0/G1 phase arrest in Huh7 cells^[5].
Eltrombopag (0.1-100 μg/mL; 72 h) exhibits anti-proliferative activity against HCC cell lines^[5]. In Vivo: Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees^[1].
Eltrombopag Olamine (17.6 mg/kg; i.p.; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection^[3].