R-138727
R-138727, the major active metabolite of Prasugrel (HY-15284), is a highly potent and selective irreversible antagonist of the P2Y12 receptor, with an IC50 of 2.5 μM. R-138727 covalently binds to the P2Y12 receptor on the platelet surface, blocking adenosine diphosphate-mediated platelet activation and aggregation. R-138727 can be used to study stroke, cerebral infarction and neurological deficits.
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- CAS No.: 204204-73-9
- Formule: C18H20FNO3S
- Masse moléculaire:349.42
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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P2Y12 Receptor 2.5 μM (IC50) |
R-138727 (0.03-100 μM; 30 min) acts as a specific antagonist for the human P2Y12 receptor expressed in CHO cells, with an IC50 of 2.5 μM for inhibiting [3H]-2-MeS-ADP binding[1].
R-138727 (0.1-10 μM; 1.5 min) potently inhibits ADP-induced aggregation in washed human platelets, with an IC50 value of 0.53 μM against 10 μM ADP and 0.63 μM against 0.1 μM 2-MeS-ADP[1].
R-138727 (0.3-30 μM; 1.5-30 min) exhibits time-dependent antiplatelet activity in human platelet-rich plasma (PRP), with its IC50 value decreasing from 28 μM (1.5 min) to 1.8 μM (30 min) as the pre-incubation time increases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:cynomolgus monkeys (male, 5-8 years old)[2]
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Dosage:0.03, 0.1, 0.3 mg/kg
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Administration:i.v.; single dose
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Result:Significantly increased total patency rate of the MCA.
Significantly reduced total ischaemic infarction volumes.
Reduced overall neurological deficits, including the subcategories of consciousnes.
Chemical Information
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CAS No. 204204-73-9
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Masse moléculaire 349.42
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Formule C18H20FNO3S
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SMILES
O=C(/C=C1CN(CCC/1S)C(C(C2CC2)=O)C3=CC=CC=C3F)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1].
Hasegawa M, et al. Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor. Thromb Haemost. 2005 Sep;94(3):593-8.
[Content Brief]
[2]. Sugidachi A, et al. The active metabolite of prasugrel, R-138727, improves cerebral blood flow and reduces cerebral infarction and neurologic deficits in a non-human primate model of acute ischaemic stroke. Eur J Pharmacol. 2016;788:132-139. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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