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. Nr.: 936501-01-8
- Formel: C20H15ClFKN5O5S2
- Molecular Weight:563.04
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
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. Further protocols information, click here.
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. Nr. 936501-01-8
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Molecular Weight 563.04
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Elinogrel potassium Related Classifications
HY-14486 Related Classifications
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