PSB-0739
Based on 1 publication(s) in Google Scholar
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.
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- 純度: 98.0%
- CAS 番号: 1052087-90-7
- 分子式: C26H17N3Na2O8S2
- 分子量:609.54
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 PSB-0739
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生物活性
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P2Y12 Receptor |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 monocytic cell line
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Concentration:10 nM, 100 nM, 1 μM, 10 μM
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Incubation Time:
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Result:Attenuated ADP-evoked responses (IC50=5.4±1.8 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats, 150-250 g, 6-8/group[4]
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Dosage:0.01, 0.03, 0.1, 0.3 mg/kg
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Administration:Intrathecal injection ( i.t.)
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Result:Displayed a dose-dependent inhibitory effect on mechanical hyperalgesia in the range of 0.01–0.1 mg/kg.
化学情報
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CAS 番号 1052087-90-7
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性状 Solid
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分子量 609.54
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分子式 C26H17N3Na2O8S2
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Color Green to dark green
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SMILES
O=S(C(C(N)=C1C2=O)=CC(NC3=CC=C(NC4=CC=CC=C4)C(S(=O)(O[Na])=O)=C3)=C1C(C5=C2C=CC=C5)=O)(O[Na])=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mil Med Res
PANX1-mediated ATP release confers FAM3A's suppression effects on hepatic gluconeogenesis and lipogenesis. [Abstract]2024 Jun 27;11(1):41. PMID: 38937853
溶剤 & 溶解度
H2O : 3.33 mg/mL (5.46 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (284 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.6406 mL | 8.2029 mL | 16.4058 mL | 41.0145 mL |
| 5 mM | 0.3281 mL | 1.6406 mL | 3.2812 mL | 8.2029 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
PSB-0739 関連分類
HY-108660 関連分類
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