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

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.

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.

609.54

C₂₆H₁₇N₃Na₂O₈S₂

1052087-90-7

固體

Green to dark green

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• [1]. Younis Baqi, et al. High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y₁₂ receptors. J Med Chem. 2009 Jun 25;52(12):3784-93.  [Content Brief]

  [2]. Kristina Hoffmann, et al. Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y₁₂ receptor. J Pharmacol Exp Ther. 2009 Nov;331(2):648-55.  [Content Brief]

  [3]. J J Micklewright,et al. P2Y 12 receptor modulation of ADP-evoked intracellular Ca²⁺ signalling in THP-1 human monocytic cells. Br J Pharmacol.2018 Jun;175(12):2483-2491.  [Content Brief]

  [4]. Gergely Horváth, et al. Central P2Y₁₂ receptor blockade alleviates inflammatory and neuropathic pain and cytokine production in rodents. Neurobiol Dis. 2014 Oct;70(100):162-78.  [Content Brief]