Avatrombopag

Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM) . Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].

Product Specifications

CAS Number

[570406-98-3]

Product Name Alternative

AKR-501; E5501; YM477

UNSPSC

12352005

Hazard Statement

H314

Target

Thrombopoietin Receptor

Type

Reference compound

Related Pathways

Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

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

Concentration

10mM

Purity

99.83

Solubility

DMSO : 8.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C29H34Cl2N6O3S2

Molecular Weight

649.65

Precautions

H314

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 Sep;12 (9) :859-865.|[3]Nomoto M, 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.