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Rivastigmine Tartrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rivastigmine Tartrate图片
CAS NO:129101-54-8
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
酒石酸卡巴拉汀
ENA 713
SDZ-ENA 713
产品介绍
Rivastigmine tartrate (ENA 713; SDZ-ENA 713) 是一种具有口服活性的,有效的胆碱酯酶 (ChE) 抑制剂,可抑制丁酰胆碱酯酶 (BChE) 和乙酰胆碱酯酶 (AChE),IC50分别为 0.037 μM 和 4.15 μM。Rivastigmine tartrate 可透过血脑屏障 (BBB)。Rivastigmine tartrate 是一种拟副交感神经剂或胆碱能剂,用于研究轻度至中度阿尔茨海默氏型痴呆和帕金森氏病引起的痴呆。
生物活性

Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potentcholinesterase (ChE)inhibitor and inhibitsbutyrylcholinesterase (BChE)andacetylcholinesteras (AChE)withIC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].

IC50& Target

IC50: 0.037 μM (BChE) and 4.15 μM (AChE)[1]

体外研究
(In Vitro)

Rivastigmine tartrate (ENA 713; 1 μM; 24 hours) reduces LPS (2.5 μg/ml)-induced TNF-α and IL-6 by 50% and 46% combined with carbachol (10 μM), respectively and does not cause any significant reduction in pro-inflammatory cytokines[3].
Rivastigmine tartrate (1 μM), carbachol (10 μM), or a combination of both drugs, does not have a cytotoxic effect on activated cells[3].

体内研究
(In Vivo)

Rivastigmine tartrate (ENA 713; 0.5-2.5 mg/kg; IP; 60 min before the tests) significantly and dose-dependently improved the behavioral impairments caused by Aluminum (HY-B1521)[4].
Rivastigmine (0.5, 1 mg/kg/day; s.c; for 8 days) reduces by about 50% and 60% respectively, the concentration of IL-6 but not those of TNF-α and IL-1β in BALB/c OlaHsd male mice aged 8-9 weeks weighing 200–250 g with acute colitis[3].
Rivastigmine (1 mg/kg), but not (0.5 mg/kg), partially antagonized colon shrinkage and completely prevented bleeding. Treatment with rivastigmine (0.5 mg/kg) causes little change in these pathological manifestations, but rivastigmine (1 mg/kg) causes a partial restoration of the structure of the crypts and a reduction in sub-mucosal edema and cell infiltration. Rivastigmine (1 mg/kg) causes a 4.7% reduction in body weight at the end of the experiment[3].

Animal Model:Male Wistar albino rats weighing 190–240 g (90 days old)[4]
Dosage:0.5, 1, 1.5 and 2.5 mg/kg
Administration:IP; single dose
Result:Significantly and dose-dependently improved the behavioral impairments caused by Aluminum (100 mg/kg/day; i.p.; for 60 days)
Clinical Trial
分子量

400.42

性状

Solid

Formula

C18H28N2O8

CAS 号

129101-54-8

中文名称

酒石酸卡巴拉汀;利斯的明酒石酸盐;卡巴拉汀酒石酸盐;酒石酸利伐斯的明;酒石酸利凡斯的明

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 50 mg/mL(124.87 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4974 mL12.4869 mL24.9738 mL
5 mM0.4995 mL2.4974 mL4.9948 mL
10 mM0.2497 mL1.2487 mL2.4974 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (249.74 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。