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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- CAS No.: 936501-01-8
- 화학식: C20H15ClFKN5O5S2
- 분자량:563.04
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of Elinogrel potassium
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
P2Y12 Receptor 20 nM (IC50) |
In Vitro
Elinogrel (PRT060128) (30 μM; 20 min) potassium serves to define and distinguish P2Y12-specific binding sites in mouse and human platelets (platelet-rich plasma or washed platelets)[2].
Elinogrel potassium exhibits high affinity for the P2Y12 receptor (Ki = 23 nM) and possesses anti-platelet aggregation activity (IC50 = 2.81 μM)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Elinogrel (1 mg/kg; i.v.; single dose; 15-minute observation) potassium abolishes residual thrombus formation in an FeCl3-induced thrombosis model in wild-type C57BL/6J mice pretreated with Clopidogrel (HY-15283) (50 mg/kg; oral; for 3 days)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type C57BL/6J mice, 10% FeCl3-induced mesenteric artery thrombosis Model[2]
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Dosage:60 mg/kg
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Administration:p.o.; twice daily; for 3 days; 40-minute post-injury observation
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Result:Provided a superior level of inhibition of thrombosis.
Reproduced the phenotype of P2Y12(-/-) mice.
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Animal Model:Clopidogrel-treated wild-type C57BL/6J mice, 10% FeCl3-induced mesenteric artery thrombosis model[2]
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Dosage:1 mg/kg
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Administration:i.v.; single dose; 15-minute observation
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Result:Eliminated the residual thrombotic process observed in clopidogrel-treated animals.
Chemical Information
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CAS No. 936501-01-8
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분자량 563.04
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화학식 C20H15ClFKN5O5S2
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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]
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Synonyms
PRT060128 potassium
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Elinogrel potassium Related Classifications
HY-14486 Related Classifications
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