1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Brevetoxin-3

Brevetoxin-3 (Synonyms: PbTx-3)

Cat. No.: HY-12545
Handling Instructions

Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.

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Brevetoxin-3 Chemical Structure

Brevetoxin-3 Chemical Structure

CAS No. : 85079-48-7

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Description

Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain)[1]. Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation[2].

IC50 & Target

IC50: voltage-gated Na+ channel[1]

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)[1].

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[3].
.

Animal Model: Pregnant CD-1 mice[3]
Dosage: 2.8 μg/kg
Administration: Intratracheal instillation; 2.8 μg/kg; gestational days 15–18
Result: Demonstrated placental transport of brevetoxin or its metabolites following maternal acute exposure. 
Molecular Weight

897.10

Formula

C₅₀H₇₂O₁₄

CAS No.

85079-48-7

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Keywords:

Brevetoxin-3PbTx-3Brevetoxin3Brevetoxin 3PbTx3PbTx 3Sodium ChannelNa channelsNa+ channelsAirwayhyperresponsivenessAHRlunginflammationactivatorInhibitorinhibitorinhibit

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Brevetoxin-3
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