Brevetoxin-3,85079-48-7

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Brevetoxin-3

CAS No. : 85079-48-7

MCE 国际站：Brevetoxin-3

产品活性：Brevetoxin-3 (PbTx-3) 是一种有效的变构电压门控 Na⁺ 通道 (Na⁺ channels) 激活剂，具有多个活性中心 (A 环内酯，R 侧链的 C-42)。Brevetoxin-3 (PbTx-3) 对电压敏感的 Na⁺ 通道的位点 5 具有高亲和力，抑制 Na⁺ 通道的失活并延长这些通道的平均打开时间。Brevetoxin-3 (PbTx-3) 可导致气道高反应性 (AHR) 延长和肺部炎症。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

In Vitro: Brevetoxin-3 (PbTx-3)(30-500 nM) produces a shift in activation to more negative membrane potentials whereby single-channel activity is observed under steady-state conditions (maintained depolarization at -50 mV).

In Vivo: Brevetoxin-3 (PbTx-3)(intratracheal instillation; 2.8 μg/kg; gestational days 15-18) radioactivity is detected in placentas and fetuses within 0.5 hours. Concentrations of brevetoxin equivalents in fetuses are approximately 0.3 ng/g throughout the 48-h post-dosing, resulting in a calculated dose to fetuses of 19 ng/gh. Following brevetoxin infusion, concentration of brevetoxin equivalents in fetuses is 0.1 ng/g, lower than that present in most maternal tissues.
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