Avatrombopag (maleate)

Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC50: 3.3 nM) . Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A [1][2][3].

Product Specifications

CAS Number

[677007-74-8]

Product Name Alternative

AKR-501 (maleate) ; E5501 (maleate) ; YM477 (maleate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Cytochrome P450; ERK; STAT; Thrombopoietin Receptor

Type

Reference compound

Related Pathways

Immunology/Inflammation; JAK/STAT Signaling; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/avatrombopag-maleate.html

Purity

99.88

Solubility

DMSO : 175 mg/mL (ultrasonic)

Smiles

O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O.O=C(O)/C=C\C(O)=O

Molecular Formula

C33H38Cl2N6O7S2

Molecular Weight

765.73

Precautions

H302, H315, H319

References & Citations

[1]Fukushima-Shintani M, et al. AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist. Eur J Haematol. 2009;82 (4) :247-254.|[2]Xu H, et al. Avatrombopag for the treatment of thrombocytopenia in patients with chronic liver disease. Expert Rev Clin Pharmacol. 2019;12 (9) :859-865.|[3]Nomoto M, Zamora CA, Schuck E, et al. Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs. Br J Clin Pharmacol. 2018;84 (5) :952-960.