Eltrombopag

Research use only, not for human use.

Eltrombopag is an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity.

Eltrombopag is an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity. Eltrombopag binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110), a member of the hematopoietin receptor superfamily. Activation of TPO-R leads to the proliferation and differentiation of megakaryocytes, thereby increasing the production of blood platelets.(In Vitro):Eltrombopag (0.002-50 μM; 4 h) possesses activity in murine BAF3 cells transfected with the luciferase reporter gene.Eltrombopag (30 μM; 120 min) affects the activates of p-STAT5 in N2C-Tpo cells.Eltrombopag (30 μM; 120 min) activates p-STAT5 in megakaryocytes.Eltrombopag (0.1 nM-10 μM; 30 min) stimulates proliferation of BAF3/hTpoR cells.Eltrombopag (0.03-3 μM; 10 days) increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes.Eltrombopag (0-3 μM; 72 h) affects N2C-Tpo cell apoptosis.Eltrombopag efficiently inhibits Pneumococcal growth with MIC50 of 0.3 mg/L, but shows no activity against Gram-negative bacteria.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.Eltrombopag (0 or 10 μg/mL; 72 h) significantly induces G0/G1 phase arrest in Huh7 cells.Eltrombopag (0.1-100 μg/mL; 72 h) exhibits anti-proliferative activity against HCC cell lines.(In Vivo):Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees.Eltrombopag Olamine (17.6 mg/kg; i.p.; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection.

Cell Viability Assay Cell Line:Murine BAF3 cells Concentration:0.002-50 μM Incubation Time:4 hResult:Effectively inhibited murine BAF3 cells with human TpoR with an EC50 value of 0.27 μM.Cell Line:N2C-Tpo cells and CD34+Concentration:30 μM for N2C-Tpo cells; 0, 1, 3 and 10 μM for CD34+Incubation Time:120 min for N2C-Tpo cells; 30 min for CD34+Result:Activated phospho-STAT5 and maximum signal intensity exhibited at 60 minutes after treatment in N2C-Tpo cells.Dose-dependently activated STAT5 phosphorylation at 30 minutes after treatment in CD34+.Cell Proliferation Assay Cell Line:BAF3/hTpoR cells Concentration:0.1 nM-10 μM Incubation Time:2 days Result:Promoted BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50 of 0.03 μM.Cell Differentiation Assay Cell Line:CD34+ Concentration:0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM Incubation Time:10 days Result:Dose-dependently stimulated the differentiation from bone marrow CD34+ cells to CD41+ megakaryocytes with an EC50 value of 0.1 μM.Apoptosis Analysis Cell Line:N2C-Tpo cells Concentration:0, 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM Incubation Time:72 hours Result:Exhibited dose-dependently antiapoptotic effects N2C-Tpo cells with a concentration over 0.03 μM.Cell Proliferation Assay Cell Line:Huh7, HepG2 and Hep3B cells (preloaded with iron (500 μg/ml FAC) for 24 h )Concentration:0.1-100 μg/mLIncubation Time:72 hResult:Exhibited anti-proliferative activity against HCC cell lines with IC50s of 5.7 μg/ml for Huh7, 5.4 μg/ml for HepG2, and 4.7 μg/ml for Hep3B.Cell Cycle Analysis Cell Line:Huh7 cells Concentration:0 or 10 μg/mL Incubation Time:72 h Result:Significantly induced G0/G1 phase arrest.

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.

SB 497115

Autophagy

Thrombin

Thrombopoietin receptor

Cardiovascular Disease

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496775-61-2

442.47

C25H22N4O4

>98% (HPLC)

DMSO: 26 mg/mL warmed (58.76 mM)

CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)N/N=C/3\C=CC=C(C3=O)C4=CC(=CC=C4)C(=O)O)C

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(-20℃)

With Ice Pack

≥ 2 years