FAAH inhibitor 1 (Synonyms: Benzothiazole analog 3) |
Catalog No.GC36023
One-Click Copy Product Info
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FAAH Inhibitor 1 is a selective, reversible inhibitor of fatty acid amide hydrolase (FAAH), with an IC50 value of 18±8nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 326866-17-5
Sample solution is provided at 25 µL, 10mM.
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FAAH Inhibitor 1 is a selective, reversible inhibitor of fatty acid amide hydrolase (FAAH), with an IC50 value of 18±8nM[1]. FAAH Inhibitor 1 exhibits no off-target activity against other serine hydrolases and is suitable for use in research on neurological disorders[2, 3]. FAAH Inhibitor 1 acts as a dual inhibitor of both FAAH and soluble epoxide hydrolase (sEH)[4].
In vivo, FAAH Inhibitor 1 (1mg/kg), administered via intraperitoneal injection in a rat model of formalin-induced acute inflammatory pain, attenuated the licking and guarding behaviors elicited by plantar formalin injection; the resulting analgesic effect was comparable to that of ketoprofen (a conventional non-steroidal anti-inflammatory drug)[4].
References:
[1] Wang X, Sarris K, Kage K, et al. Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors[J]. Journal of medicinal chemistry, 2009, 52(1): 170-180.
[2] Dider S, Ji J, Zhao Z, et al. Molecular mechanisms involved in the side effects of fatty acid amide hydrolase inhibitors: a structural phenomics approach to proteome-wide cellular off-target deconvolution and disease association[J]. NPJ systems biology and applications, 2016, 2(1): 16023.
[3] Papa A, Pasquini S, Contri C, et al. Polypharmacological approaches for CNS diseases: focus on endocannabinoid degradation inhibition[J]. Cells, 2022, 11(3): 471.
[4] Wilt S, Kodani S, Valencia L, et al. Further exploration of the structure-activity relationship of dual soluble epoxide hydrolase/fatty acid amide hydrolase inhibitors[J]. Bioorganic & medicinal chemistry, 2021, 51: 116507.
| Animal experiment [1]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were removed from their home cages and briefly anesthetized with isoflurane. A dilute formalin solution (5%, 50µL) was then injected into the plantar surface of the right hindpaw. Rats were placed on an elevated mesh rack for observation. The amount of time spent licking or guarding the injected hindpaw was measured in seconds in 5min blocks for one hour following hindpaw injection. FAAH inhibitor 1 was dissolved in DMSO to a stock concentration of 10mM. The 10mM stock was further diluted into injectable doses (0.1 and 1.0mg/kg) using a vehicle solution comprising 10% ethanol, 10% cremophor, and 80% saline. Ketoprofen was dissolved in the same vehicle. Drugs were injected intraperitoneally in a volume of 1mL/kg. All drugs were administered 30min before hindpaw injection of formalin. |
Dosage form | 0.1, 1mg/kg; i.p. |
Applications | Intraperitoneal administration of the higher dose of FAAH inhibitor 1 attenuates licking and guarding behaviors induced by an intraplantar injection of formalin. The lower dose of FAAH inhibitor 1 was ineffective suggesting a dose-dependent relationship in antinociception. The magnitude of antinociception produced by 1mg/kg of FAAH inhibitor 1 is comparable to antinociception produced by a high dose of ketoprofen (30mg/kg). |
References: | |
| Cas No. | 326866-17-5 | SDF | |
| Synonyms | Benzothiazole analog 3 | ||
| Canonical SMILES | CC1=CC=C(N=C(C2=CC=C(NC(C3CCN(S(=O)(C4=CC=CS4)=O)CC3)=O)C=C2)S5)C5=C1 | ||
| Formula | C24H23N3O3S3 | M.Wt | 497.65 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C,protect from light |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0094 mL | 10.0472 mL | 20.0944 mL |
| 5 mM | 401.9 μL | 2.0094 mL | 4.0189 mL |
| 10 mM | 200.9 μL | 1.0047 mL | 2.0094 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)