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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
Rivastigmine Tartrate
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
129101-54-8
- 规格:
200mg/100mg/50mg
| 规格: | 200mg | 产品价格: | ¥1190.0 |
|---|---|---|---|
| 规格: | 100mg | 产品价格: | ¥890.0 |
| 规格: | 50mg | 产品价格: | ¥590.0 |
| 基本信息 | |
| CAS | No.129101-54-8 |
| 中文名称 | 酒石酸卡巴拉汀 |
| 英文名称 | Rivastigmine Tartrate |
| 别名 | 酒石酸卡巴拉汀;利斯的明酒石酸盐; |
| 分子式 | C18H28N2O8 |
| 分子量 | 400.42 |
| 溶解性 | Soluble in Water/DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| MDL | MFCD03700731 |
| SMILES | CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O |
| InChIKey | GWHQHAUAXRMMOT-MBANBULQSA-N |
| InChI | InChI=1S/C14H22N2O2.C4H6O6/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4;5-1(3(7)8)2(6)4(9)10/h7-11H,6H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t11-;1-,2-/m01/s1 |
| PubChem CID | 6918078 |
| 靶点 | AChE;BChE |
| 通路 | Neuronal Signaling |
| 背景说明 | 是一种有效的胆碱酯酶 (ChE) 抑制剂,可抑制丁酰胆碱酯酶 (BChE) 和乙酰胆碱酯酶 (AChE)。 |
| 生物活性 | Rivastigmine Tartrate 是一种口服活性强效胆碱酯酶(ChE)抑制剂,可抑制丁酰胆碱酯酶(BChE)和乙酰胆碱酯酶(AChE),其 IC50 值分别为 0.037 μM 和 4.15 μM,可用于研究阿尔茨海默型痴呆和帕金森病所致痴呆。 |
| IC50 | BChE: 0.037μM(IC50);AChE: 4.15μM(IC50)[1] |
| In Vitro | In combination with carbachol(10 μM),Rivastigmine Tartrate(1 μM)significantly decreased the release of nitric oxide,TNF-α,IL-1β and IL-6 from lipopolysaccharide-activated RAW 264.7 macrophages.[2] |
| 细胞实验 | Rivastigmine Tartrate(1 mg/kg,injected subcutaneously,once daily)in DSS mice reduced the disease activity index(DAI)by 60% and damage to colon structure. Rivastigmine Tartrate(1 mg/kg)also reduced myeloperoxidase activity and IL-6 by >60%,and the infiltration of CD11b expressing cells by 80%. These effects were accompanied by significantly greater ChE inhibition in cortex,brain stem,plasma and colon than that after 0.5 mg/kg. Co-administration of Rivastigmine Tartrate(1 mg/kg)with the muscarinic antagonist scopolamine significantly increased the number of CD11b expressing cells in the colon but did not change DAI compared to those treated with Rivastigmine Tartrate alone.[2] Rivastigmine Tartrate can reverse behavioral deficits caused by aluminum intoxication. The behavioral impairments of rats caused by aluminum were significantly improved by Rivastigmine Tartrate,the maximal improvement was encountered with its large dose(2.5 mg/kg).[3] |
| 动物实验 | Rats were exposed to aluminum chloride(100 mg/kg/day i.p.)for 60 days before the start of behavioral tests. Rivastigmine Tartrate was given in doses of 0.5,1,1.5 and 2.5 mg/kg i.p. 60 min before the behavioral tests. Five tests were investigated; open field test,Morris water maze,radial arm maze,passive avoidance test and rota-rod test.[3] |
| 数据来源文献 | [1]. Yu QS,et al. Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. J Med Chem. 2002 Aug 15;45(17):3684-91. [2]. Shifrin H,et al. Rivastigmine alleviates experimentally induced colitis in mice and rats by acting at central and peripheral sites to modulate immune responses. PLoS One. 2013;8(2):e57668. [3]. Abdel-Aal RA,et al. Rivastigmine reverses aluminum-induced behavioral changes in rats. Eur J Pharmacol. 2011 Jun 1;659(2-3):169-76. |
| 单位 | 瓶 |
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