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(-)-p-Bromotetramisole Oxalate

现货
Catalog No.
B4750
ALP抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
10mg
¥ 670.00
现货
50mg
¥ 1,650.00
现货

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Background

(-)-p-Bromotetramisole Oxalate (L-(-)-p-Bromotetramisole Oxalate, L-p-Bromotetramisole Oxalate, (-)-4-Bromotetramisole Oxalate) is a potent and non-specific inhibitor of alkaline phosphatase and is also an inhibitor of protein tyrosine phosphatases [1] [2].

Alkaline phosphatase is a hydrolase enzyme that removes phosphate groups from nucleotides, proteins and alkaloids. Protein tyrosine phosphatase is an enzyme that removes phosphate groups from phosphorylated tyrosine residues on target proteins.

(-)-p-Bromotetramisole Oxalate is an inhibitor of alkaline phosphatase and protein tyrosine phosphatases. In various rat tissues, (-)-p-Bromotetramisole Oxalate (0.1 μM) completely inhibited non-specific alkaline phosphatase [1]. In rat zona glomerulosa, (-)-p-Bromotetramisole Oxalate (100 μM) blocked the inhibition of Na+ pump (Na+, K+-ATPase) induced by angiotensin II. The result suggested that inhibition of the Na+ pump induced by angiotensin II might be mediated by a tyrosine phosphatase [2]. In neurosecretory PC12 cells, (-)-p-Bromotetramisole Oxalate (0.3 mM) increased ionomycin-stimulated noradrenaline (NA) release, which suggested that tyrosine phosphorylation regulated Ca2+-stimulated NA release [3].

In Sprague-Dawley rats, (-)-p-Bromotetramisole Oxalate (10 μM) significantly increased fractional excretion of phosphate (FEPi) from 4.7% to 13.4% [4].

References:
[1].  Borgers M, Thoné F. The inhibition of alkaline phosphatase by L-p-bromotetramisole. Histochemistry, 1975, 44(3): 277-280.
[2].  Yingst DR, Davis J, Schiebinger R. Inhibitors of tyrosine phosphatases block angiotensin II inhibition of Na(+) pump. Eur J Pharmacol, 2000, 406(1): 49-52.
[3].  Kitamura T, Murayama T, Nomura Y. Enhancement of Ca2+-induced noradrenaline release by vanadate in PC12 cells: possible involvement of tyrosine phosphorylation. Brain Res, 2000, 854(1-2): 165-171.
[4].  Onsgard-Meyer M, McCoy AL, Knox FG. Effect of bromotetramisole on renal phosphate excretion. Proc Soc Exp Biol Med, 1996, 213(2): 193-195.

Chemical Properties

StorageDesiccate at -20°C
M.Wt373.22
Cas No.62284-79-1
FormulaC13H13BrN2O4S
Solubility≥18.65mg/mL in DMSO
SDFDownload SDF
Canonical SMILESBrC(C=C1)=CC=C1[C@H]2N=C3SCCN3C2.OC(C(O)=O)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

神经分泌PC12细胞

溶解方法

在DMSO中的溶解度>18.7mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0.3 mM

应用

在神经分泌PC12细胞中,(-)-p-Bromotetramisole Oxalate显著增强PC12细胞中5μM离子霉素刺激的[3H] NA释放。(-)-p-Bromotetramisole Oxalate单独使用仅轻微刺激[3H] NA释放。

动物实验[2]:

动物模型

甲状腺手术切除Sprague-Dawley大鼠

剂量

10 mM (-)-p-Bromotetramisole Oxalate;以0.8ml / min全身输注

应用

在甲状腺手术切除的Sprague-Dawley大鼠中,(-)-p-Bromotetramisole Oxalate显著增加磷酸盐(FEPi)的排泄分数,从4.7%±0.9%增加至13.4%±3.1%。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Kitamura T, Murayama T, Nomura Y. Enhancement of Ca2+-induced noradrenaline release by vanadate in PC12 cells: possible involvement of tyrosine phosphorylation. Brain Res, 2000, 854(1-2): 165-171.

[2]. Onsgard-Meyer M, McCoy AL, Knox FG. Effect of bromotetramisole on renal phosphate excretion. Proc Soc Exp Biol Med, 1996, 213(2): 193-195.

生物活性

Description (-)-p-Bromotetramisole Oxalate是一种有效的和非特异性的碱性磷酸酶抑制剂.
靶点 alkaline phosphatase          
IC50            

质量控制

化学结构

(-)-p-Bromotetramisole Oxalate