936501-01-8
Chemical Structure
Elinogrel potassium
Synonym(s): PRT060128 potassium
- CAS No.: 936501-01-8
- Formula:C20H15ClFKN5O5S2
- Molecular Weight:563.04
IUPAC Name: 5-chloro-N-((4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)phenyl)carbamoyl)thiophene-2-sulfonamide, potassium salt
InChIKey: ORAKJDGBKULZRH-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(Cl)S1)(NC(NC2=CC=C(N3C(NC4=C(C=C(F)C(NC)=C4)C3=O)=O)C=C2)=O)=O.[K]
Biological Activity: Elinogrel (PRT060128) potassium is an orally active, selective, competitive, and reversible direct-acting platelet P2Y12 antagonist (IC50 = 20 nM). Elinogrel potassium blocks ADP-induced signaling by directly and reversibly competing for binding to the platelet P2Y12 receptor. Elinogrel potassium exhibits rapid and potent anti-platelet aggregation and antithrombotic activities. Elinogrel potassium is suitable for research into acute coronary syndrome and antithrombotic[1][2][3][4].
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Elinogrel potassium | Elinogrel (PRT060128) potassium is an orally active, selective, competitive, and reversible direct-acting platelet P2Y12 antagonist (IC50 = 20 nM). Elinogrel potassium blocks ADP-induced signaling by directly and reversibly competing for binding to the platelet P2Y12 receptor. Elinogrel potassium exhibits rapid and potent anti-platelet aggregation and antithrombotic activities. Elinogrel potassium is suitable for research into acute coronary syndrome and antithrombotic. | |||||||||||||||||||||
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References
- [1]. Angiolillo DJ, et al. Pharmacokinetic and pharmacodynamic effects of elinogrel: results of the platelet function substudy from the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in nonurgent percutaneous coronary intervention patients (INNOVATE-PCI) trial. Circ Cardiovasc Interv. 2012 Jun;5(3):347-56. [Content Brief]
- [2]. Haberstock-Debic H, et al. A clopidogrel-insensitive inducible pool of P2Y12 receptors contributes to thrombus formation: inhibition by elinogrel, a direct-acting, reversible P2Y12 antagonist. J Pharmacol Exp Ther. 2011 Oct;339(1):54-61. [Content Brief]
- [3]. Jacobson KA, et al. Pharmacochemistry of the platelet purinergic receptors. Purinergic Signal. 2011 Sep;7(3):305-24. [Content Brief]
- [4]. Zech G, et al. Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone. J Med Chem. 2012 Oct 25;55(20):8615-29. [Content Brief]
