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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C33H27NO8 |
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分子量 | 565.57 | CAS No. | 475205-49-3 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (176.81 mM) | ||||||||
Ethanol | 100 mg/mL (176.81 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | A-317491 is a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors with Ki values of 22 nM and 9 nM for human P2X3 and P2X2/3 receptors. |
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in vitro | A-317491 potently blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and is highly selective (IC50 >10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 does not undergo any detectable metabolism (oxidation or glucuronidation) in in vitro assays using human and rat liver microsomes[1]. |
in vivo | A-317491 dose-dependently (ED50 = 30 μmol/kg s.c.) reduces complete Freund's adjuvant-induced thermal hyperalgesia in the rat. A-317491 is most potent (ED50 = 10-15 μmol/kg s.c.) in attenuating both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury. Although active in chronic pain models, A-317491 is ineffective (ED50 >100 μmol/kg s.c.) in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain. Preliminary pharmacokinetic studies in rats indicate that 10 μmol/kg A-317491 had high (≈80%) systemic bioavailability after s.c. dosing (estimated plasma concentration = 15 μg/ml, >99% protein bound) and a half-life in plasma of 11 h[1]. A-317491 is effective in reducing pain associated behavior in several animal models of inflammatory and neuropathic pain when administered systemically. A-317491 does not significantly penetrate into the CNS[2]. |
動物実験 | 動物モデル | male Sprague-Dawley rats |
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投薬量 | 3, 10 and 30 mg/kg | |
投与方法 | s.c. |
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長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。