1257792-42-9
Chemical Structure
Rafutrombopag diolamine
- CAS No.: 1257792-42-9
- Formula:C29H36N6O7
- Molecular Weight:580.64
IUPAC Name: 2-aminoethan-1-ol hemi((Z)-5-(2-hydroxy-3-(2-(3-methyl-5-oxo-1-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,5-dihydro-4H-pyrazol-4-ylidene)hydrazinyl)phenyl)furan-2-carboxylate)
InChIKey: LEXFXZIVRDMLHQ-SBIAVEDLSA-N
SMILES: O=C1N(N=C(/C1=N/NC2=C(C(C3=CC=C(C(O)=O)O3)=CC=C2)O)C)C4=CC=C(CCCC5)C5=C4.NCCO.NCCO
Biological Activity: Rafutrombopag (Hetrombopag) diolamine is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag diolamine can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag diolamine specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag diolamine effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag diolamine protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag diolamine can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease[1][2][3].
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Rafutrombopag diolamine | Rafutrombopag (Hetrombopag) diolamine is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag diolamine can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag diolamine specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag diolamine effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag diolamine protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag diolamine can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease. | |||||||||||||||||||||
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- [1]. Xie C, et al. Pharmacological characterization of hetrombopag, a novel orally active human thrombopoietin receptor agonist. J Cell Mol Med. 2018 Nov;22(11):5367-5377. [Content Brief]
- [2]. Zhou N, et al. Hetrombopag, a Thrombopoietin Receptor Agonist, Protects Cardiomyocyte Survival from Oxidative Stress Damage as an Enhancer of Stem Cells. Cardiovasc Drugs Ther. 2016 Dec;30(6):567-577. [Content Brief]
- [3]. Zhao Yufei MD, et al. Hetrombopag, an Emerging Iron-Chelating Agent, Alleviates Systemic Iron Overload. 2024 Nov. Page 3848, ISSN 0006-4971.
Keywords
