| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TC-F2 targets fatty acid amide hydrolase (FAAH), a serine hydrolase that hydrolyzes endogenous fatty acid amides including anandamide, oleamide, and palmitoylethanolamide. FAAH is the principal enzyme responsible for terminating the signaling of these lipid messengers. By inhibiting FAAH, TC-F2 increases the levels of endocannabinoids and other fatty acid amides, modulating pain, inflammation, and other physiological processes. TC-F2 is a reversible, non-covalent inhibitor with an IC₅₀ of 28 nM for human FAAH.
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| ln Vitro |
TC-F2 inhibits human FAAH with an IC₅₀ of 28 nM and rat FAAH with an IC₅₀ of 100 nM. It is a reversible, non-covalent binding inhibitor. FAAH inhibition by TC-F2 increases endocannabinoid levels, which can modulate pain, inflammation, and other physiological processes. The compound is used as a research tool to study FAAH biology and the endocannabinoid system. Specific in vitro efficacy data in cell-based assays are not extensively documented.
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| ln Vivo |
In vivo activity data for TC-F2 are limited in the literature. Based on its potent in vitro FAAH inhibition, it is anticipated to have potential in vivo efficacy in models of pain, inflammation, and other FAAH-related conditions. However, specific animal studies detailing its therapeutic effects, dosing, and pharmacokinetics are not extensively documented.
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| Enzyme Assay |
The non-cellular enzyme/receptor binding assay for TC-F2 typically involves measuring FAAH enzymatic activity using a fluorometric or radiometric assay. Recombinant FAAH enzyme is incubated with a substrate (e.g., anandamide or a fluorogenic substrate) and varying concentrations of TC-F2. The hydrolysis of the substrate is measured over time. IC₅₀ values are calculated from dose-response curves. Selectivity over other serine hydrolases can be assessed using similar assays with panels of related enzymes.
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| Cell Assay |
In vitro cellular assays for TC-F2 typically use cell lines expressing FAAH to evaluate enzyme inhibition. Cells are treated with various concentrations of TC-F2, and FAAH activity is assessed by measuring the hydrolysis of a fluorogenic substrate or by quantifying anandamide levels using LC-MS/MS. Cell viability is assessed using MTT or LDH assays. The compound's effects on downstream endocannabinoid signaling can be evaluated by measuring relevant signaling markers.
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| Animal Protocol |
In vivo animal studies for TC-F2 are not extensively documented. Based on its FAAH inhibitory mechanism, typical study designs would involve rodent models of pain (e.g., formalin test, hot plate test), inflammation (e.g., carrageenan-induced paw edema), or other FAAH-related conditions. TC-F2 would be administered orally or intraperitoneally. Efficacy endpoints would include pain thresholds, inflammatory markers, and endocannabinoid levels in tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TC-F2 are not extensively characterized. As a small molecule with molecular weight 439.51, it is expected to have reasonable oral bioavailability. The compound likely crosses the blood-brain barrier given its target in the central nervous system. Metabolic pathways likely involve hepatic cytochrome P450-mediated oxidation. Specific PK parameters such as half-life, Cmax, and protein binding are not well documented.
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| Toxicity/Toxicokinetics |
Toxicological data for TC-F2 are limited. As a research-grade compound, comprehensive toxicology studies are not available. The compound has been used in research settings without reports of significant acute toxicity. However, detailed toxicity profiles are not documented. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
TC-F2 is a research-grade compound intended for laboratory use only. It is not approved for clinical use as a therapeutic agent. Its primary applications include studying FAAH biology and the endocannabinoid system, investigating the role of FAAH in pain, inflammation, cancer, and neurological, metabolic, and cardiovascular diseases, and exploring the therapeutic potential of FAAH inhibitors. TC-F2 is a valuable tool for neuroscience and drug discovery research.
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| Molecular Formula |
C26H25N5O2
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|---|---|
| Molecular Weight |
439.509005308151
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| Exact Mass |
439.201
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| CAS # |
1304778-15-1
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| PubChem CID |
25198728
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| Appearance |
White to off-white solid powder
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| LogP |
4.932
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
706
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCN1C2=CC=CC=C2N(C1=O)[C@H]3CCCN(C3)C4=NC=CC(=N4)C5=CC6=CC=CC=C6O5
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| InChi Key |
NXTBLPPTZRPJCA-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C26H25N5O2/c1-2-30-21-10-4-5-11-22(21)31(26(30)32)19-9-7-15-29(17-19)25-27-14-13-20(28-25)24-16-18-8-3-6-12-23(18)33-24/h3-6,8,10-14,16,19H,2,7,9,15,17H2,1H3/t19-/m0/s1
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| Chemical Name |
1-[(3S)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethylbenzimidazol-2-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~568.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.73 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2753 mL | 11.3763 mL | 22.7526 mL | |
| 5 mM | 0.4551 mL | 2.2753 mL | 4.5505 mL | |
| 10 mM | 0.2275 mL | 1.1376 mL | 2.2753 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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