Hydroxytacrine (maleate) (Synonyms: HP 029,1-Hydroxytacrine,P 83-6029A,Velnacrine) |
| Catalog No.GC15604 |
anticholinesterase activity
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118909-22-1
Sample solution is provided at 25 µL, 10mM.
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Hydroxytacrine maleate, a bioactive monohydroxylated metabolite of cholinesterase inhibitor, is a potential Alzheimer's therapeutic of low toxicity [1]. Hydroxytacrine maleate exhibited biochemical and pharmacological profile similar to tacrine (THA) except that the far less liver toxicity in humans. The prolonged use of tacrine has been associated with liver toxicity[1, 2].
Hydroxytacrine maleate is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). As the first cholinesterase inhibitor approved for the treatment of AD, tacrine was marketed under the trade name Cognex [3]. Through hydroxylation of benzylic carbon by CYP450 in the liver, tacrine has been metabolized into metabolite 1-hydroxy-tacrine (velnacrine) [4]. It has also been shown that maleate is an inhibitor of AChE [5].
References:
[1]. D. Muoz-Torrero. Acetylcholinesterase inhibitors as disease-modifying therapies for Alzheimer’s disease. Curr. Med. Chem. 15, 2433-2455 (2008).
[2]. E. Giacobini. Cholinesterase inhibitors for Alzheimer’s disease therapy: From tacrine to future applications. Neurochemistry International 32, 413-419(1998).
[3]. Birks J S. Cholinesterase inhibitors for Alzheimer's disease[J]. The Cochrane Library, 2006.
[4]. Peng J Z, Remmel R P, Sawchuk R J. Inhibition of murine cytochrome P4501A by tacrine: in vitro studies[J]. Drug metabolism and disposition, 2004, 32(8): 805-812.
[5]. Acetylcholine and choline effects on erythrocyte nitrite and nitrate levels.
| Cas No. | 118909-22-1 | SDF | |
| Sinónimos | HP 029,1-Hydroxytacrine,P 83-6029A,Velnacrine | ||
| Chemical Name | 9-amino-1,2,3,4-tetrahydro-1-acridinol, 2Z-butenedioate | ||
| Canonical SMILES | NC1=C2C(CCCC2O)=NC3=CC=CC=C31.OC(/C=C\C(O)=O)=O | ||
| Formula | C13H14N2O • C4H4O4 | M.Wt | 330.3 |
| Solubility | ≤30mg/ml in DMSO;2mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0276 mL | 15.1378 mL | 30.2755 mL |
| 5 mM | 0.6055 mL | 3.0276 mL | 6.0551 mL |
| 10 mM | 0.3028 mL | 1.5138 mL | 3.0276 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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