Eltrombopag

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

艾曲波帕是一种口服活性血小板生成素受体激动剂，具有巨核细胞生成刺激活性。

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