| Identification | Back Directory | [Name]
5-Chloro-N-[[[4-[6-fluoro-1,4-dihydro-7-(methylamino)-2,4-dioxo-3(2H)-quinazolinyl]phenyl]amino]carbonyl]-2-thiophenesulfonamide | [CAS]
936500-94-6 | [Synonyms]
elinogrel
PRT 060128
P2Y Receptor,inhibit,PRT 060128,Elinogrel,Inhibitor,PRT-060128
5-Chloro-N-[[[4-[6-fluoro-1,4-dihydro-7-(MethylaMino)-2,4-dioxo-3(2H)-quinazolinyl]phenyl]aMino]carb
5-Chloro-N-[[[4-[6-fluoro-1,4-dihydro-7-(methylamino)-2,4-dioxo-3(2H)-quinazolinyl]phenyl]amino]carbonyl]-2-thiophenesulfonamide
2-Thiophenesulfonamide, 5-chloro-N-[[[4-[6-fluoro-1,4-dihydro-7-(methylamino)-2,4-dioxo-3(2H)-quinazolinyl]phenyl]amino]carbonyl]- | [Molecular Formula]
C20H15ClFN5O5S2 | [MDL Number]
MFCD16619373 | [MOL File]
936500-94-6.mol | [Molecular Weight]
523.95 |
| Chemical Properties | Back Directory | [density ]
1.651 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100 mM | [form ]
A solid | [pka]
4.42±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Elinogrel is a reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 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 |
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