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187269-40-5

中文名稱 Bimosiamose
英文名稱 Bimosiamose
CAS 187269-40-5
分子式 C46H54O16
分子量 862.92
MOL 文件 187269-40-5.mol
187269-40-5 結(jié)構(gòu)式 187269-40-5 結(jié)構(gòu)式

基本信息

中文別名
比莫西糖
英文別名
TBC-1269
Bimosiamose
[1,1'-Biphenyl]-3-acetic acid, 3',3'''-(1,6-hexanediyl)bis[6'-(α-D-mannopyranosyloxy)-

物理化學(xué)性質(zhì)

熔點(diǎn)115-117°
沸點(diǎn)1051.0±65.0 °C(Predicted)
密度1.417±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO:100.0(Max Conc. mg/mL);115.89(Max Conc. mM)
0.1 M NaOH:25.0(Max Conc. mg/mL);28.97(Max Conc. mM)
酸度系數(shù)(pKa)3.95±0.10(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
Bimosiamose (TBC-1269) 是一種非寡糖泛-selectin 拮抗劑,對 E-selectin,P-selectin 和 L-selectin 的 IC50 分別為 88 μM,20 μM 和 86μM。Bimosiamose 具有抗炎作用。
靶點(diǎn)

IC50: 88 μM (E-selectin), 20 μM (P-selectin), 86 μM (L-selectin)

體外研究

Bimosiamose (TBC-1269) operates by inhibiting neutrophil recruitment to the site of inflammation through blocking the initial rolling phase of recruitment. Bimosiamose (TBC-1269) inhibits cell recruitment and does not possess any cytotoxic effect on neutrophils.

體內(nèi)研究

Bimosiamose (TBC-1269; 25 mg/kg; intravenous injection; Sprague-Dawley rats) treatment shows a significant increase in survival. Best overall survival, 70%, is observed when TBC-1269 is administered 15 minutes before reperfusion, and also shows a marked decrease in liver enzyme levels at 6 hours after reperfusion. Neutrophil migration is also significantly ameliorated (81%). The histologic damage scores is also improved.

Animal Model: Sprague-Dawley rats (200-225g) with ischemia and reperfusion (I/R)
Dosage: 25 mg/kg
Administration: Intravenous injection
Result: Showed a significant increase in survival compared with controls.
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