Rafutrombopag

Rafutrombopag (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].

Product Specifications

CAS Number

[2600513-51-5]

Product Name Alternative

Hetrombopag; SHR-8735

UNSPSC

12352005

Target

Apoptosis; CDK; ERK; PI3K; STAT; Thrombopoietin Receptor

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Immunology/Inflammation; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/rafutrombopag.html

Solubility

10 mM in DMSO

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

Molecular Formula

C25H22N4O5

Molecular Weight

458.47

References & Citations

[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.|[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.|[3]Zhao Yufei MD, et al. Hetrombopag, an Emerging Iron-Chelating Agent, Alleviates Systemic Iron Overload. 2024 Nov. Page 3848, ISSN 0006-4971.