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 番号: 204204-73-9
- 分子式: C18H20FNO3S
- 分子量:349.42
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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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.
化学情報
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CAS 番号 204204-73-9
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分子量 349.42
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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