2114365-78-3
Chemical Structure
Rafutrombopag (tautomerism)
Synonym(s): Hetrombopag (tautomerism);SHR-8735 (tautomerism)
- CAS No.: 2114365-78-3
- Formula:C25H22N4O5
- Molecular Weight:458.47
IUPAC Name: (E)-5-(2-hydroxy-3-((3-methyl-5-oxo-1-(5,6,7,8-tetrahydronaphthalen-2-yl)-4,5-dihydro-1H-pyrazol-4-yl)diazenyl)phenyl)furan-2-carboxylic acid
InChIKey: WTZFEDHEXDVDRO-CYYJNZCTSA-N
SMILES: O=C(C1=CC=C(C2=C(O)C(/N=N/C3C(N(C4=CC=C5C(CCCC5)=C4)N=C3C)=O)=CC=C2)O1)O
Biological Activity: Rafutrombopag (tautomerism) (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag 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 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 protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease[1][2][3].
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Rafutrombopag (tautomerism) | 98.33% | Rafutrombopag (tautomerism) (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag 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 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 protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag 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]. Zhao Yufei MD, et al. Hetrombopag, an Emerging Iron-Chelating Agent, Alleviates Systemic Iron Overload. 2024 Nov. Page 3848, ISSN 0006-4971.
- [3]. https://pubmed.ncbi.nlm.nih.gov/30156363/ [Content Brief]
Keywords
