| Identification | Back Directory | [Name]
PSB 0739 | [CAS]
1052087-90-7 | [Synonyms]
PSB 0739
PSB 0739, CID59448166
1-Amino-9,10-dihydro-9,10-dioxo-4-[[4-(phenylamino)-3-sulfophenyl]amino]-2-anthracenesulfonic acid sodium salt
sodium 1-amino-9,10-dioxo-4-{[4-(phenylamino)-3-[(sodiooxy)sulfonyl]phenyl]amino}-9,10-dihydroanthracene-2-sulfonate | [Molecular Formula]
C26H20N3NaO8S2 | [MDL Number]
MFCD22683797 | [MOL File]
1052087-90-7.mol | [Molecular Weight]
589.57 |
| Chemical Properties | Back Directory | [Melting point ]
>300 °C | [storage temp. ]
Desiccate at RT | [form ]
Powder | [color ]
Green to dark green | [Water Solubility ]
Soluble to 25 mM in water |
| Hazard Information | Back Directory | [Description]
Highly potent P2Y12receptor antagonist (Ki= 24.9 nM). Unlike clopidogrel, does not require bioactivation. | [Uses]
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 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: | 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.
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| [IC 50]
P2Y12 Receptor | [storage]
Desiccate at RT | [References]
[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. DOI:10.1021/jm9003297
[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. DOI:10.1124/jpet.109.156687
[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. DOI:10.1111/bph.14218
[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. DOI:10.1016/j.nbd.2014.06.011 |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
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