PSB-0739

SKU: orb3027361

Description

PSB-0739 is a potent, competitive, and selective P2Y12 receptor antagonist with a Ki of 24.9 nM. It is a valuable research tool for studying platelet aggregation mechanisms and evaluating antithrombotic strategies in both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1052087-90-7
• MW: 609.54
• Formula: C₂₆H₁₇N₃Na₂O₈S₂
• SMILES: O=C1C2=C(C(C3=C(NC4=CC=C(C(S(=O)([O-])=O)=C4)NC5=CC=CC=C5)C=C(S(=O)([O-])=O)C(N)=C13)=O)C=CC=C2.[Na+].[Na+]
• Target: P2Y Receptor
• Solubility: H2O:1 mg/mL (1.64 mM)

Bioactivity

• Target IC50:
  HIV-1 infection enhanced by SEVI:21.77 μM
• In Vivo:
  In rat models, PSB-0739 administered intrathecally (0.01–0.3 mg/kg) significantly reduced CFA-induced inflammatory pain and sciatic nerve ligation-induced neuropathic pain, with a minimal effective dose of 0.1 mg/kg. It also increased pain thresholds in the hot plate test, indicating analgesic effects. Additionally, PSB-0739 decreased the expression of pro-inflammatory cytokines such as IL-1β and TNF-α in inflamed tissues (paw and spinal cord), suggesting its mechanism involves inhibition of cytokine signaling both centrally and peripherally.
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• In Vitro:
  PSB-0739 inhibits the formation of semen-derived amyloid fibrils (SEVI), which enhance HIV-1 infection. It demonstrates direct anti-HIV activity with an IC₅₀ of 21.77 ± 5.15 μM, without significant cytotoxicity in HeLa cells at concentrations below 62.5 μM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PSB 0739, PSB0739, PSB-0739

Quick Database Links

Gene Symbol

P2Y Receptor