2. GPCR/G Protein Metabolic Enzyme/Protease
  3. P2Y Receptor Drug Metabolite
  4. 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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R-138727

R-138727 Chemical Structure

CAS No. : 204204-73-9

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R-138727 Related Antibodies

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Description

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.

IC50 & Target[1]

P2Y12 Receptor

2.5 μM (IC50)

In Vitro

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.

R-138727 Related Antibodies
In Vivo

R-138727 (0.03-0.3 mg/kg; intravenous injection; single dose) exerts dose-dependent antiplatelet effects in a non-human primate model of ischemic stroke, increases the recanalization rate of the middle cerebral artery (MCA), reduces cerebral infarction volume, and improves neurological deficits[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: cynomolgus monkeys (male, 5-8 years old)[2]
Dosage: 0.03, 0.1, 0.3 mg/kg
Administration: i.v.; single dose
Result: Significantly increased total patency rate of the MCA.
Significantly reduced total ischaemic infarction volumes.
Reduced overall neurological deficits, including the subcategories of consciousnes.
Molecular Weight

349.42

Formula

C18H20FNO3S
CAS No.
SMILES

O=C(/C=C1CN(CCC/1S)C(C(C2CC2)=O)C3=CC=CC=C3F)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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R-138727 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R-138727204204-73-9R138727R 138727P2Y ReceptorDrug Metabolitewashed human plateletsADPnon-human primate model of acute ischaemic strokehuman P2Y? receptorsCHO cellshuman P2Y?? receptorprasugrel2-MeS-ADPmiddle cerebral arteryhuman platelet-rich plasmaInhibitorinhibitorinhibit

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