(R)-Rivastigmine D6 tartrate
(Synonyms: 酒石酸卡巴拉汀 D6) 目录号 : GC34993
An internal standard for the quantification of rivastigmine
Cas No.:194930-00-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rivastigmine-d6 is intended for use as an internal standard for the quantification of rivastigmine by GC- or LC-MS. Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyrl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).1 It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.2 In a rat model of Alzheimer's disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.3 It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer's disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.4 Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer's disease and Parkinson's disease.
1.Yu, Q.S., Zhu, X., Holloway, H.W., et al.Anticholinesterase activity of compounds related to geneserine tautomers. N-oxides and 1,2-oxazinesJ. Med. Chem.45(17)3684-3691(2002) 2.Bailey, J.A., Ray, B., Greig, N.H., et al.Rivastigmine lowers Aβ and increases sAPPα levels, which parallel elevated synaptic markers and metabolic activity in degenerating primary rat neuronsPLoS One6(7)e21954(2011) 3.Ismail, M.F., Elmeshad, A.N., and Salem, N.A.Potential therapeutic effect of nanobased formulation of rivastigmine on rat model of Alzheimer's diseaseInt. J. Nanomedicine8393-406(2013) 4.Papp, M., Gruca, P., Lason-Tyburkiewicz, M., et al.Antidepressant, anxiolytic and procognitive effects of rivastigmine and donepezil in the chronic mild stress model in ratsPsychopharmacology (Berl)233(7)1235-1243(2016)
| Cas No. | 194930-00-2 | SDF | |
| 别名 | 酒石酸卡巴拉汀 D6 | ||
| Canonical SMILES | O=C(OC1=CC=CC([C@@H](C)N(C([2H])([2H])[2H])C([2H])([2H])[2H])=C1)N(CC)C.O=C(O)[C@H](O)[C@@H](O)C(O)=O | ||
| 分子式 | C18H22D6N2O8 | 分子量 | 406.46 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 16 mg/ml,Ethanol: 16 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4603 mL | 12.3013 mL | 24.6027 mL |
| 5 mM | 0.4921 mL | 2.4603 mL | 4.9205 mL |
| 10 mM | 0.246 mL | 1.2301 mL | 2.4603 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。