PSB-0739_product_DataBase

Bioactivity	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].
Invitro	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]. Cell Viability Assay[3] Cell Line:
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]. Animal Model:
Name	PSB-0739
CAS	1052087-90-7
Formula	C26H17N3Na2O8S2
Molar Mass	609.54
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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. [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. [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. [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.

PeptideDB

PSB-0739

CAS: 1052087-90-7 F: C26H17N3Na2O8S2 W: 609.54