AM 1172 |
| カタログ番号GC12972 |
アナンダミドの取り込みとFAAHの阻害剤、強力で選択的
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 251908-92-6
Sample solution is provided at 25 µL, 10mM.
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AM 1172 is a potent and selective inhibitor of stable anandamide uptake with IC50 of 2.1 - 2.5 μM and fatty acid amide hydrolase (FAAH) with Ki of 3.18 μM.
FAAH, a member of serine hydrolase enzyme family, is an integral membrane hydrolase that hydrolyzes bioactive amides, including anandamide, to free fatty acid and ethanolamine. In vitro, FAAH displays esterase and amidase activity. In vivo, this protein acts as the principal catabolic enzyme for a class of bioactive lipids called the fatty acid amides (FAAs).
AM1172 blocked [3H] anandamide internalization in rodent cortical neurons and human astrocytoma cells but not acted as an inhibitor of FAAH 1. In mouse cortical neurons, This component also blocked the uptake of tritiated AEA with an EC50 of about 1.5 µM 1.
Regarding the effect of AM 1172 administration in vivo, the evidence should be provided by performing the study in human or mice or other animal models.
Reference:
1. Fegley D, Kathuria S, Mercier R, et al. Anandamide transport is independent of fatty-acid amide hydrolase activity and is blocked by the hydrolysis-resistant inhibitor AM1172. Proceedings of the National Academy of Sciences of the United States of America. 2004;101(23):8756-8761.
| Cas No. | 251908-92-6 | SDF | |
| Chemical Name | 4-hydroxy-N-((5E,8E,11E,14E)-icosa-5,8,11,14-tetraen-1-yl)benzamide | ||
| Canonical SMILES | O=C(C(C=C1)=CC=C1O)NCCCC/C=C/C/C=C/C/C=C/C/C=C/CCCCC | ||
| Formula | C27H39NO2 | M.Wt | 409.6 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): .15 mg/ml | 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. |
||
| 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 | 2.4414 mL | 12.207 mL | 24.4141 mL |
| 5 mM | 0.4883 mL | 2.4414 mL | 4.8828 mL |
| 10 mM | 0.2441 mL | 1.2207 mL | 2.4414 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 37 reference(s) in Google Scholar.)
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