Rafutrombopag (tautomerism)

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].

Product Specifications

CAS Number

[2114365-78-3]

Product Name Alternative

Hetrombopag (tautomerism) ; SHR-8735 (tautomerism)

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

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

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

Purity

98.33

Solubility

DMF : 6.25 mg/mL (ultrasonic; warming; heat to 60°C) |DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

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

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]https://pubmed.ncbi.nlm.nih.gov/30156363/|[3]Zhao Yufei MD, et al. Hetrombopag, an Emerging Iron-Chelating Agent, Alleviates Systemic Iron Overload. 2024 Nov. Page 3848, ISSN 0006-4971.