5-Chloro-N-[[[4-[6-fluoro-1,4-dihydro-7-(methylamino)-2,4-dioxo-3(2H)-quinazolinyl]phenyl]amino]carbonyl]-2-thiophenesulfonamide

Description

Elinogrel is a reversible antagonist of the platelet purinergic P2Y₁₂ receptor (K_i = 23 nM) that inhibits platelet aggregation in a human platelet-rich plasma (hPRP) assay (IC₅₀ = 2.81 nM). It inhibits thrombosis in a mouse model of vascular injury induced by iron (III) chloride (FeCl₃) when administered at a dose of 60 mg/kg.

Uses

Elinogrel is a direct acting reversible P2Y12 inhibitor, which shows an antiplatelet effect and platelet reactivity associated with cytochrome P 450 2C19 and 3A5 gene polymorphisms.

IC 50

P2Y12 Receptor

storage

Store at -20°C

References

[1] GERNOT ZECH. Identification of High-Affinity P2Y12 Antagonists Based on a Phenylpyrazole Glutamic Acid Piperazine Backbone[J]. Journal of Medicinal Chemistry, 2012, 55 20: 8615-8629. DOI: 10.1021/jm300771j
[2] HELENA HABERSTOCK-DEBIC. A clopidogrel-insensitive inducible pool of P2Y12 receptors contributes to thrombus formation: inhibition by elinogrel, a direct-acting, reversible P2Y12 antagonist.[J]. ACS Applied Electronic Materials, 2011: 54-61. DOI: 10.1124/jpet.111.184143