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溴代新斯的明 /Neostigmine bromide {[allProObj[0].p_purity_real_show]}

货号:A198984 同义名: 溴化新斯的明 / Eustigmin bromide;Neoserine bromide

Neostigmine bromide is a cholinesterase inhibitor used in the treatment of myasthenia gravis. Neostigmine bromide is a reversible AchR inhibitor but can not cross the blood-brain barrier.

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Type HazMat fee for 500 gram (Estimated)
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Neostigmine bromide 化学结构 CAS号:114-80-7
Neostigmine bromide 化学结构
CAS号:114-80-7
Neostigmine bromide 3D分子结构
CAS号:114-80-7
Neostigmine bromide 化学结构 CAS号:114-80-7
Neostigmine bromide 3D分子结构 CAS号:114-80-7
规格 价格 会员价 库存 数量
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Neostigmine bromide 纯度/质量文件 产品仅供科研

货号:A198984 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 nM

98%
Loganin ++

AChE, IC50: 3.95 μM

99%+
topride HCl ++

AChE, IC50: 2.04 μM

98%
Dehydroevodiamine HCl 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

99%+
Palmatine ++

AChE, IC50: 0.51 μM

98%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 98+%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 98%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine hydrochloride 97%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 98%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

98%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Neostigmine bromide 生物活性

靶点
  • AChR

描述 Neostigmine bromide is a reversible acetylcholine esterase inhibitor that binds to the anionic binding site of AChE. Administration of neostigmine, may successfully reverse some negative effects of inflammation on the GnRH (gonadotropin-releasing hormone) neurons[3]. As the molecular weight of neostigmine bromide is 303 g/mol and the steady-state volume of distribution is approximately 0.5 L/kg, its plasma concentration was calculated to be 0.13–0.46 μM. The dosage of neostigmine can be reduced properly when used to antagonize the residual neuromuscular block in septic patients[4].

Neostigmine bromide 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03399890 - Completed - Turkey ... 展开 >> Ankara University Faculty of Medicine Ankara, Turkey 收起 <<
NCT03519633 Curarization, Postoperative Re... 展开 >>sidual 收起 << Phase 2 Not yet recruiting January 30, 2019 Italy ... 展开 >> Campus Bio-medico Recruiting Roma, RM, Italy, 00128 Contact: Corrado Terranova    06225411203 ext +39    c.terranova@unicampus.it 收起 <<
NCT03519724 Curarization, Postoperative Re... 展开 >>sidual 收起 << Phase 2 Not yet recruiting January 30, 2019 Italy ... 展开 >> Campus Bio-medico Recruiting Roma, RM, Italy, 00128 Contact: Corrado Terranova    06225411203 ext +39    c.terranova@unicampus.it 收起 <<

Neostigmine bromide 参考文献

[1]Khorshid AF, Issa YM. Modified carbon paste sensor for the potentiometric determination of neostigmine bromide in pharmaceutical formulations, human plasma and urine. Biosens Bioelectron. 2014 Jan 15;51:143-9.

[2]Trevisani GT, Hyman NH, et al. Neostigmine: safe and effective treatment for acute colonic pseudo-obstruction. Dis Colon Rectum. 2000 May;43(5):599-603.

[3]Herman AP, Tomaszewska-Zaremba D, Kowalewska M, Szczepkowska A, Oleszkiewicz M, Krawczyńska A, Wójcik M, Antushevich H, Skipor J. Neostigmine Attenuates Proinflammatory Cytokine Expression in Preoptic Area but Not Choroid Plexus during Lipopolysaccharide-Induced Systemic Inflammation. Mediators Inflamm. 2018 Oct 9;2018:9150207.

[4]Wu J, Jin T, Wang H, Li ST. Sepsis Strengthens Antagonistic Actions of Neostigmine on Rocuronium in a Rat Model of Cecal Ligation and Puncture. Chin Med J (Engl). 2016 Jun 20;129(12):1477-82.

Neostigmine bromide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.49mL

3.30mL

1.65mL

32.98mL

6.60mL

3.30mL

Neostigmine bromide 技术信息

CAS号114-80-7
分子式C12H19BrN2O2
分子量 303.195
别名 溴化新斯的明 ;Eustigmin bromide;Neoserine bromide
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 105 mg/mL(346.31 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(329.82 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 80 mg/mL clear

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