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

Brevetoxin-3  (Synonyms: PbTx-3)

Cat. No.: HY-12545 Purity: ≥95.0%
COA 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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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](C[C@@]3([H])[C@@](C)(CC[C@@]4([H])[C@]([C@@H](C[C@@]5([H])[C@](C[C@@]6(C)[C@](C[C@@](O7)([H])[C@](C(C)=CC7=O)([H])O6)([H])O5)([H])O4)C)([H])O3)O2)([H])O[C@]8(C)[C@@](O[C@]9([H])[C@@](O[C@]%10([H])[C@@](O[C@]%11(C)[C@@](O[C@H](CC(CO)=C)C[C@@H]%11O)([H])C%10)([H])C9)([H])/C=C\C8)([H])C1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥95.0%

References
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Brevetoxin-3 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Brevetoxin-3
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