Rivastigmine tartrate (Synonyms:酒石酸卡巴拉汀; ENA 713; SDZ-ENA 713)
目录号 : KM8211 CAS No. : 129101-54-8 纯度 : 98%

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。

规格 价格 是否有货 数量
50mg
In-stock
100mg
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200mg
In-stock
500mg 询价 In-stock
1g 询价 In-stock

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生物活性

Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s 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.

体外研究

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 .
Rivastigmine tartrate (1 µM), carbachol (10 µM), or a combination of both drugs, does not have a cytotoxic effect on activated cells.

体内研究

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 .
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.
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.

Animal Model: Male Wistar albino rats weighing 190–240 g (90 days old)
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)
分子式
C14H22N2O2.C4H6O6
分子量
400.42
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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 mg 5 mg 10 mg
1 mM 2.4974 mL 12.4869 mL 24.9738 mL
5 mM 0.4995 mL 2.4974 mL 4.9948 mL
10 mM 0.2497 mL 1.2487 mL 2.4974 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°C, 6 months; -20°C, 1 month。-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。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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