(-)-p-Bromotetramisole Oxalate
(Synonyms: (-)-对溴四咪唑草酸盐; L-p-Bromotetramisole oxalate; 6-Bromolevamisole oxalate) 目录号 : GC14520
(-)-p-Bromotetramisole Oxalate是强效的非特异性的碱性磷酸酶抑制剂。
Cas No.:62284-79-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment [1]: |
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Cell lines |
PC12 cells |
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Preparation method |
The prelabeled PC12 cells were incubated with vehicle or 5 μM ionomycin in the presence of 2 mM CaCl2. (-)-p-Bromotetramisole Oxalate (BTO) was further added to the assay mixture. |
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Reaction Conditions |
0.3 mM |
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Applications |
(-)-p-Bromotetramisole Oxalate enhances ionomycin-stimulated norepinephrine (NA) release. |
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Animal experiment [2]: |
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Animal models |
Sprague-Dawley rats |
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Preparation method |
Rats were anesthetized and pretreated with propranolol to prevent norepinephrine-induced activation of β-adrenoceptors. 2 cannulas were inserted into the jugular vein (one for administration of norepinephrine and the other for administration of l-p-bromotetramisole). An IV infusion of 0.9% saline (50 μL/min) was initiated to maintain volume status. After a 30-minute stabilization period, rats were treated with either 2 IV slow-bolus injections (separated by 15 minutes) of vehicle (saline) or(-)-p-Bromotetramisole Oxalate (total dose, 30 mg/kg). Administering the (-)-p-Bromotetramisole Oxalate as 2 slow injections minimized basal blood pressure perturbations. Fifteen minutes after the second bolus of (-)-p-Bromotetramisole Oxalate, norepinephrine was infused at 10 μg/kg/min for 10 minutes. |
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Dosage form |
30 mg/kg; ivgtt |
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Applications |
(-)-p-Bromotetramisole Oxalate significantly inhibited norepinephrine-induced mean arterial blood pressure (MABP) elevation and renal vascular resistance. |
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References: [1]. Kitamura T, Murayama T, et,al. Enhancement of Ca2+-induced noradrenaline release by vanadate in PC12 cells: possible involvement of tyrosine phosphorylation. Brain Res. 2000 Jan 31;854(1-2):165-71. doi: 10.1016/s0006-8993(99)02299-4. PMID: 10784118. [2]. Jackson EK, Zhang Y, et,al. Alkaline Phosphatase Inhibitors Attenuate Renovascular Responses to Norepinephrine. Hypertension. 2017 Mar;69(3):484-493. doi: 10.1161/HYPERTENSIONAHA.116.08623. Epub 2017 Jan 30. PMID: 28137984; PMCID: PMC5310812. |
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(-)-p-Bromotetramisole Oxalate(L-p-bromotetramisole) is a potent and non-specific inhibitor of alkaline phosphatase [1-2].
(-)-p-Bromotetramisole Oxalate (1 mM) augmented cAMP-stimulated iodide efflux and, by itself, stimulated a larger efflux than that evoked by cAMP agonists, suggesting that it may promote the opening of humancystic fibrosis transmembrane conductance regulator (CFTR) in CHO cells[3]. In PC12 cells, (-)-p-Bromotetramisole Oxalate (0.3 mM) enhances ionomycin-stimulated norepinephrine (NA) release[4].
(-)-p-Bromotetramisole Oxalate(30 mg/kg; ivgtt) significantly inhibited norepinephrine-induced MABP elevation and renal vascular resistance. It reduces renal vascular and blood pressure response to norepinephrine[5]. Systemic infusion of (-)-p-Bromotetramisole Oxalate (0.8 ml/min of 10 mM I-p-Bromotetramisole oxalate; ivgtt) increases Fractional excretion of phosphate (FEPi) in Sprague-Dawley rats[6].
References:
[1]. Borgers M. The cytochemical application of new potent inhibitors of alkaline phosphatases. J Histochem Cytochem. 1973 Sep;21(9):812-24. doi: 10.1177/21.9.812. PMID: 4741290.
[2]. Borgers M, Thoné F. The inhibition of alkaline phosphatase by L-p-bromotetramisole. Histochemistry, 1975, 44(3): 277-280.
[3]. Lansdell KA, Kidd JF, et,al. Regulation of murine cystic fibrosis transmembrane conductance regulator Cl- channels expressed in Chinese hamster ovary cells. J Physiol. 1998 Nov 1;512 ( Pt 3)(Pt 3):751-64. doi: 10.1111/j.1469-7793.1998.751bd.x. PMID: 9769419; PMCID: PMC2231228.
[4]. Kitamura T, Murayama T, et,al. Enhancement of Ca2+-induced noradrenaline release by vanadate in PC12 cells: possible involvement of tyrosine phosphorylation. Brain Res. 2000 Jan 31;854(1-2):165-71. doi: 10.1016/s0006-8993(99)02299-4. PMID: 10784118.
[5]. Jackson EK, Zhang Y,et,al. Alkaline Phosphatase Inhibitors Attenuate Renovascular Responses to Norepinephrine. Hypertension. 2017 Mar;69(3):484-493. doi: 10.1161/HYPERTENSIONAHA.116.08623. Epub 2017 Jan 30. PMID: 28137984; PMCID: PMC5310812.
[6]. Onsgard-Meyer M, McCoy AL, et,al. Effect of bromotetramisole on renal phosphate excretion. Proc Soc Exp Biol Med. 1996 Nov;213(2):193-5. doi: 10.3181/00379727-213-44050. PMID: 8931664.
(-) -P-Bromotetramisole Oxalate是一种有效的非特异性碱性磷酸酶抑制剂[1-2]。
(-) -P-Bromotetramisole Oxalate(1 mM)增强了cAMP刺激的碘化物外排，且其本身刺激的外排量大于cAMP激动剂引起的外排量，提示其可能促进CHO细胞中人囊性纤维化跨膜传导调节剂(CFTR)的开放[3]。(-) -P-Bromotetramisole Oxalate(0.3 mM)可增强PC12细胞的离子霉素刺激的去甲肾上腺素(NA) [4]。
(-) -P-Bromotetramisole Oxalate (30mg /kg; ivgtt)显著抑制去甲肾上腺素诱导的平均动脉血压升高和肾血管阻力。它能降低肾血管和血压对去甲肾上腺素的反应[5]。在大鼠中全身输注(-) -P-Bromotetramisole Oxalate(0.8 ml/min of 10 mM (-) -P-Bromotetramisole Oxalate; ivgtt)可增加磷酸的部分排泄(FEPi) [6]。
| Cas No. | 62284-79-1 | SDF | |
| 别名 | (-)-对溴四咪唑草酸盐; L-p-Bromotetramisole oxalate; 6-Bromolevamisole oxalate | ||
| Canonical SMILES | BrC(C=C1)=CC=C1[C@H]2N=C3SCCN3C2.OC(C(O)=O)=O | ||
| 分子式 | C13H13BrN2O4S | 分子量 | 373.22 |
| 溶解度 | ≥ 18.65mg/mL in DMSO | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6794 mL | 13.3969 mL | 26.7938 mL |
| 5 mM | 0.5359 mL | 2.6794 mL | 5.3588 mL |
| 10 mM | 0.2679 mL | 1.3397 mL | 2.6794 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。