Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :Eltrombopag Olamine496775-62-3HY-15306A5.63C29H36N6O6>98%Solubility:DMSOMechanisms: Pathways:Others; Target:Thrombopoietin Receptor Biological Activity:Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulatesthrombopoiesis. IC50 Value: 0.27 uM (EC50 in murine BAF3 cells) [1] Target: thrombopoietin-receptor (c-mpl) Potential advantages of eltrombopag may include a sustained platelet response and a goodtolerability profile. in vitro: Eltrombopag demonstrated a half maximal effective concentration (EC50) of 0.27 uM inmurine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR) [1]. Eltrombopag stimulates thegrowthofTPO-dependentgrowth of TPOdependent cell lines via JAK2 and STAT signaling pathways and stimulates isolatedcelllinesviaJAK2andSTATsignalingpathwaysandstimulatesisolatedhuman CD34+ cells to become megakaryocytes and produce platelets [2]. in vivo: Twelve weeks of antiviral therapy, with concurrent receipt of eltrombopag or placebo, werecompleted by 36...References:[1]. Erickson-Miller CL, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptidethrombopoietin receptor agonist. Stem Cells. 2009 Feb;27(2):424-30. [2]EricksonMillerCLetalDiscoveryandcharacterizationofaselectivenonpeptidyl[2]. Erickson-Miller CL, et al. Discovery and characterization of a selective, nonpeptidylthrombopoietin receptor agonist. Exp Hematol. 2005 Jan;33(1):85-93. [3]. McHutchison JG, et al. Eltrombopag for thrombocytopenia in patients with cirrhosis associatedwith hepatitis C. N Engl J Med. 2007 Nov 29;357(22):2227-36. [4]. Jenkins JM, et al. Phase 1 clinical study of eltrombopag, an oral, nonpeptide thrombopoietinreceptor agonist. Blood. 2007 Jun 1;109(11):4739-41. [5]. Saleh MN, et al. Safety and efficacy of eltrombopag for treatment of chronic immunethrombocytopenia: results of the long-term, open-label EXTEND study. Blood. 2013 Jan17;121(3):537-45. ...Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
