Eltrombopag

Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator. It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor and stimulates megakaryocytopoiesis in human primary bone marrow cells. It increases platelet production in chimpanzees when administered at a dose of 10 mg/kg per day for five days. Eltrombopag also binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells in a concentration-dependent manner. It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Cay-16753) and CP40.Formal Name: 3'-[2-[(2Z)-1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid. CAS Number: 496775-61-2. Synonyms: SB 497115. Molecular Formula: C25H22N4O4. Formula Weight: 442.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 20 mg/ml, Ethanol: 0.1 mg/ml, PBS (pH 7.2): Slightly. lambdamax: 248, 417 nm. SMILES: OC1=C(N/N=C2C(N(C3=CC(C)=C(C)C=C3)N=C\2C)=O)C=CC=C1C4=CC(C(O)=O)=CC=C4. InChi Code: InChI=1S/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,26,30H,1-3H3,(H,32,33)/b27-22-. InChi Key: XDXWLKQMMKQXPV-QYQHSDTDSA-N.