Eltrombopag

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Eltrombopag

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Cat No: 13247

Biochemicals - Receptor Pharmacology

Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.{16951} It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

nonpeptide non-peptide agonist megakaryopoiesis thrombopoietin TPO-R TPOR CD110 CD-110 496775-62-3 platelet thrombocytopenia rINN JAK-STAT JAKSTAT SB497115

Product Overview:
Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.{16951} 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.{47035} It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Item No. 16753) and CP40.

Size	1 mg
Shipping	dry ice
CAS Number	496775-61-2
Molecular Formula	C₂₅H₂₂N₄O₄
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
Molecular Weight	442,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2928.00
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.