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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Store at 2-8℃,2 years
- 保质期:
Store at 2-8℃,2 years
- 英文名:
Rivastigmine
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
123441-03-2
- 规格:
200mg/25mg/10mg/100mg/50mg
| 规格: | 200mg | 产品价格: | ¥1190.0 |
|---|---|---|---|
| 规格: | 25mg | 产品价格: | ¥370.0 |
| 规格: | 10mg | 产品价格: | ¥230.0 |
| 规格: | 100mg | 产品价格: | ¥890.0 |
| 规格: | 50mg | 产品价格: | ¥590.0 |
| 基本信息 | |
| CAS | No.123441-03-2 |
| 中文名称 | 利凡斯的明 |
| 英文名称 | Rivastigmine |
| 别名 | 卡巴拉汀;利凡斯的明;利斯的明; |
| 分子式 | C14H22N2O2 |
| 分子量 | 250.34 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Liquid |
| 储存条件 | Store at 2-8℃,2 years |
| 密度 | 1.038g/mL |
| MDL | MFCD00871496 |
| SMILES | CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C |
| InChIKey | XSVMFMHYUFZWBK-NSHDSACASA-N |
| InChI | InChI=1S/C14H22N2O2/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4/h7-11H,6H2,1-5H3/t11-/m0/s1 |
| PubChem CID | 77991 |
| 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 是一种口服活性胆碱酯酶(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。可穿过血脑屏障(BBB),可用于研究阿尔茨海默型和帕金森病引起的痴呆。[1-3] |
| IC50 | BChE: 0.037μM(IC50);AChE: 4.15μM(IC50)[1] |
| 细胞实验 | In combination with carbachol(10 μM),rivastigmine(1 μM)significantly decreased the release of nitric oxide,TNF-α,IL-1β and IL-6 from lipopolysaccharide-activated RAW 264.7 macrophages and this effect was abolished by α7 nicotinic receptor blockade by bungarotoxin. Rivastigmine(1 mg/kg/d,injected subcutaneously,DSS mice),reduced the disease activity index(DAI)by 60% and damage to colon structure. Rivastigmine(1 mg/kg)reduced myeloperoxidase activity and IL-6 by >60%,and the infiltration of CD11b expressing cells by 80%. Rivastigmine(1 mg/kg)with scopolamine significantly increased the number of CD11b expressing cells in the colon. Rivastigmine 1 and 2 mg given rectally to DNBS rats caused a dose related reduction in ChE activity in blood and colon,the number of ulcers and area of ulceration,levels of TNF-α and in MPO activity.[2] The behavioral impairments caused by aluminum were significantly improved by rivastigmine(0.5,1,1.5 and 2.5 mg/kg i.p. 60 min),and the maximal improvement was encountered with its large dose(2.5 mg/kg).[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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