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85079-48-7

中文名稱 BREVETOXIN PBTX-3
英文名稱 BREVETOXIN PBTX-3
CAS 85079-48-7
分子式 C50H72O14
分子量 897.1
MOL 文件 85079-48-7.mol
85079-48-7 結(jié)構(gòu)式 85079-48-7 結(jié)構(gòu)式

基本信息

中文別名
短裸甲藻毒素3
化合物 T10609
英文別名
PBTX-3
toxint-17
Gb 3 toxin
BREVETOXIN3
PUMILIOTOXIN
brevetoxint17
BREVETOXIN PBTX-3
DIHYDROBREVETOXIN B
BKMHDYJRAAJTAD-RXUQWMQDSA-N
42-Hydroxy-42-deoxobrevetoxin B

物理化學(xué)性質(zhì)

密度1.190±0.06 g/cm3(Predicted)
儲存條件-20C
溶解度DMSO: soluble,Ethanol: soluble,Methanol: soluble
酸度系數(shù)(pKa)13.78±0.70(Predicted)
形態(tài)固體
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS06,GHS09
警示詞危險
危險性描述H300-H410
危險品運輸編號3172
RTECS號XW5885000
危險等級6.1(a)
包裝類別I

常見問題列表

生物活性
Brevetoxin-3 (PbTx-3) 是一種有效的變構(gòu)電壓門控 Na+ 通道 (Na+?channels) 激活劑,具有多個活性中心 (A 環(huán)內(nèi)酯,R 側(cè)鏈的 C-42)。Brevetoxin-3 (PbTx-3) 對電壓敏感的 Na+ 通道的位點 5 具有高親和力,抑制 Na+ 通道的失活并延長這些通道的平均打開時間。Brevetoxin-3 (PbTx-3) 可導(dǎo)致氣道高反應(yīng)性 (AHR) 延長和肺部炎癥。
靶點

IC50: voltage-gated Na + channel

體外研究

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).

體內(nèi)研究

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. .

Animal Model: Pregnant CD-1 mice
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.
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