Description: Irreversible P2Y12 antagonist; antiplatelet and orally active
Alternative Names: LY640315, CS 747, Effient
Chemical Name: 2-[2-(Acetyloxy)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl)ethanone
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Irreversible P2Y12 antagonist; metabolised to active metabolite R-99224 (IC50 = 45 μM) irreversibly binds platelet P2Y12 receptors, inhibiting platelet activation. Antiplatelet and antithrombotic. Orally active and active in vivo. Note - inactive in vitro.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
37.34
100
Preparing Stock Solutions
The following data is based on the product molecular weight 373.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.68 mL
13.39 mL
26.78 mL
5 mM
0.54 mL
2.68 mL
5.36 mL
10 mM
0.27 mL
1.34 mL
2.68 mL
50 mM
0.05 mL
0.27 mL
0.54 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Sugidachiet al (2000) The in vivo pharmacological profile of CS-747, a novel antiplatelet agent with platelet ADP receptor antagonist properties. Br.J.Pharmacol. 129 1439 PMID: 10742300
Hashimoto
(2007) The influence of P2Y12 receptor deficiency on the platelet inhibitory activities of prasugrel in a mouse model: evidence for specific inhibition of P2Y12 receptors by prasugrel. Biochem.Pharmacol. 74 1003 PMID: 17681285
Huberet al (2009) Prasugrel. Nat.Rev.Drug Discov. 8 449 PMID: 19483707