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PSB-0739 Selective platelet P2Y12 receptor antagonist characterized by competitive binding and high affinity (Ki =24.9 nM) with antithrombotic and platelet aggregation modulating effects.
Description | PSB-0739 Selective platelet P2Y12 receptor antagonist characterized by competitive binding and high affinity (Ki =24.9 nM) with antithrombotic and platelet aggregation modulating effects. |
Targets&IC50 | HIV-1 infection enhanced by SEVI:21.77 μM |
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[1]. |
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[2]. |
Alias | PSB0739 |
Molecular Weight | 609.54 |
Formula | C26H17N3Na2O8S2 |
Cas No. | 1052087-90-7 |
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+] |
Relative Density. | no data available |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||
Solubility Information | H2O: 1.00 mg/mL (1.64 mM), Sonication is recommended. | ||||||||||
Solution Preparation Table | |||||||||||
H2O
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