产品
编 号：F364613
分子式：C33H27NO8
分子量：565.57
分子式：C33H27NO8
分子量：565.57
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 475205-49-3
产品详情
生物活性：
A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
体内研究：
A-317491 (0.1-30 mg/kg；单次皮下注射) 剂量依赖性地逆转大鼠的炎性机械痛觉过敏。 A-317491 (3-30 mg/kg；单次皮下注射) 表现出血浆半衰期 (7.38 h)、清除率 (1.83 L/h/kg) 和分布容积 (0.17 L/kg)。Animal Model:Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant
Dosage:0.1, 1, 3, 10, 30 mg/kg
Administration:A single s.c.
Result:Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration.
体外研究：
A-317491 有效阻断重组人和大鼠 P2X3 和 P2X2/3 受体介导的钙流 (Ki=22-92 nM)。 A-317491 (1 nM-10 μM) 产生浓度依赖性的背根神经节 (DRG) 电流阻滞，IC50 15 nM。
A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
体内研究：
A-317491 (0.1-30 mg/kg；单次皮下注射) 剂量依赖性地逆转大鼠的炎性机械痛觉过敏。 A-317491 (3-30 mg/kg；单次皮下注射) 表现出血浆半衰期 (7.38 h)、清除率 (1.83 L/h/kg) 和分布容积 (0.17 L/kg)。Animal Model:Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant
Dosage:0.1, 1, 3, 10, 30 mg/kg
Administration:A single s.c.
Result:Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration.
体外研究：
A-317491 有效阻断重组人和大鼠 P2X3 和 P2X2/3 受体介导的钙流 (Ki=22-92 nM)。 A-317491 (1 nM-10 μM) 产生浓度依赖性的背根神经节 (DRG) 电流阻滞，IC50 15 nM。
产品资料
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