1. GPCR/G Protein
  2. P2Y Receptor
  3. PSB-0739

PSB-0739 

Cat. No.: HY-108660
Handling Instructions

PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect.

For research use only. We do not sell to patients.

PSB-0739 Chemical Structure

PSB-0739 Chemical Structure

CAS No. : 1052087-90-7

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Description

PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect[1].

In Vitro

PSB-0739 is a potent competitive non-nucleotide antagonist at the human P2Y12 receptor with a pA2 value of 9.8[2].
PSB-0739 inhibits ADP-evoked Ca2+ responses with an EC50 of 5.4±1.8 μM and causes a rightward parallel shift in the ADP concentration–response curve in THP-1 cells[3].

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

Cell Viability Assay[3]

Cell Line: THP-1 monocytic cell line
Concentration: 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time:
Result: Attenuated ADP-evoked responses (IC50=5.4±1.8 μM).
In Vivo

PSB-0739 (0.01-0.3 mg/kg, intrathecally) has dose-dependent and significant antihyperalgesic effect in low doses. The minimal effective dose (mED) is 0.1 mg/kg[4].

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

Animal Model: Male Wistar rats, 150-250 g, 6-8/group[4]
Dosage: 0.01, 0.03, 0.1, 0.3 mg/kg
Administration: Intrathecal injection ( i.t.)
Result: Displayed a dose-dependent inhibitory effect on mechanical hyperalgesia in the range of 0.01–0.1 mg/kg.
Molecular Weight

609.54

Formula

C₂₆H₁₇N₃Na₂O₈S₂

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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PSB-0739
Cat. No.:
HY-108660
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