Palmitoyl Serotonin |
| Catalog No.GC12097 |
TRPV1 channel inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 212707-51-2
Sample solution is provided at 25 µL, 10mM.
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Palmitoyl Serotonin is a TRPV1 antagonist with IC50 value of 0.76 μM for human TRPV1 [1].
The transient receptor potential vanilloid-type 1 (TRPV1) channel is a nonselective cation channel that may be activated by a variety of exogenous and endogenous physical and chemical stimuli. TRPV1 is decreased in the injured nerve fibers but increased in those proximal to the site damage. TRPV1 is a potential new target for the development of analgesic and anti-inflammatory drugs [1].
Palmitoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is a dual antagonist of TRPV1 and fatty acid amide hydrolase (FAAH) with IC50 values of 0.27 and 8 μM, respectively. Arachidonoyl serotonin was highly effective against both acute and chronic peripheral pain [1][2]. In TRPV1 and FAAH assays, Palmitoyl serotonin inhibited anandamide hydrolysis mediated by FAAH and capsaicin-induced intracellular Ca2+ elevation in HEK293 cells overexpressing the human recombinant TRPV1 receptor with IC50 values of > 50 μM and 0.76 μM, respectively. However, the effects of replacing the arachidonoyl portion with the saturated 16-carbon palmitoyl moiety had not been studied [1].
References:
[1]. Ortar G, Cascio MG, De Petrocellis L, et al. New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. J Med Chem. 2007 Dec 27;50(26):6554-69.
[2]. Maione S, De Petrocellis L, de Novellis V, et al. Analgesic actions of N-arachidonoyl-serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors. Br J Pharmacol. 2007 Mar;150(6):766-81.
| Cas No. | 212707-51-2 | SDF | |
| Chemical Name | N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-hexadecanamide | ||
| Canonical SMILES | CCCCCCCCCCCCCCCC(NCCC1=CNC2=CC=C(O)C=C12)=O | ||
| Formula | C26H42N2O2 | M.Wt | 414.6 |
| Solubility | ≤30mg/ml in ethanol;15mg/ml in DMSO;30mg/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. |
||
| 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 | 2.412 mL | 12.0598 mL | 24.1196 mL |
| 5 mM | 0.4824 mL | 2.412 mL | 4.8239 mL |
| 10 mM | 0.2412 mL | 1.206 mL | 2.412 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 19 reference(s) in Google Scholar.)
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