| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
FAAH-IN-2 targets fatty acid amide hydrolase (FAAH), a serine hydrolase that catalyzes the hydrolysis of fatty acid amides including anandamide, oleoylethanolamide (OEA), and palmitoylethanolamide (PEA). By inhibiting FAAH, it increases the levels of these endogenous lipid signaling molecules.
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| ln Vitro |
FAAH-IN-2 is a novel and potent FAAH (fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2. It is also named as O-Desmorpholinopropyl Gefitinib and is a metabolite of gefitinib, which is an EGFR inhibitor. FAAHs (also known as EC 3.5.1.99, oleamide hydrolase, anandamide amidohydrolase) are a family of enzymes that belong to serine hydrolases. In humans, the family is represented by FAAH 1 and 2. It was first shown to break down anandamide in 1993. In humans, it is encoded by the gene FAAH.
FAAH-IN-2 inhibits FAAH activity, leading to increased levels of endocannabinoids and other fatty acid amides. This enhances endocannabinoid signaling and produces analgesic, anti-inflammatory, and anxiolytic effects in preclinical models. Detailed IC50 values for FAAH inhibition have been characterized in enzymatic assays. |
| ln Vivo |
In vivo, FAAH inhibitors have demonstrated analgesic, anti-inflammatory, and anxiolytic effects in animal models. By increasing endocannabinoid levels, they modulate pain, inflammation, and emotional responses. FAAH-IN-2 has potential utility in studying the endocannabinoid system and developing therapies for pain and anxiety disorders.
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| Enzyme Assay |
Cell-free FAAH assays for FAAH-IN-2 utilize purified recombinant FAAH enzyme and fluorescent or radiometric substrates (e.g., anandamide or arachidonoyl-7-amino-4-methylcoumarin amide). The hydrolysis reaction is performed in the presence of increasing concentrations of the compound. Enzyme activity is measured, and IC50 values are determined from concentration-response curves.
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| Cell Assay |
Cells expressing FAAH (e.g., neuronal cells, macrophages) are treated with FAAH-IN-2 at various concentrations. Endocannabinoid levels (anandamide, 2-AG) are measured by LC-MS/MS. FAAH activity in cell lysates is assessed using fluorescent substrates. Downstream signaling (e.g., CB1 receptor activation) is assessed by measuring cAMP levels or ERK phosphorylation.
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| Animal Protocol |
In vivo animal studies for FAAH-IN-2 are conducted in rodent models of pain, inflammation, and anxiety. The compound is administered via intraperitoneal or oral routes. Pain responses are assessed using hot plate, von Frey, or formalin tests. Anxiety-like behavior is assessed using elevated plus maze or open field tests. Endocannabinoid levels in brain tissue are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of FAAH-IN-2 have not been comprehensively reported. As a small molecule, it is expected to have reasonable membrane permeability and potential for central nervous system penetration. The compound is soluble in DMSO. Detailed PK parameters remain to be determined.
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| Toxicity/Toxicokinetics |
Toxicity data for FAAH-IN-2 are limited. As a FAAH inhibitor, standard toxicological assessments would be required for development. FAAH inhibitors are generally well-tolerated, though they have potential for CNS effects due to increased endocannabinoid signaling.
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| References |
WO/2008/100977A2
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| Additional Infomation |
O-Desmorpholinopropyl belongs to the quinazoline class of compounds.
FAAH-IN-2 (CAS#: 184475-71-6) is a potent and selective inhibitor of fatty acid amide hydrolase (FAAH). It is used as a research tool for studying the endocannabinoid system and the role of fatty acid amides in pain, inflammation, and emotional regulation. The compound is intended for research use only. |
| Molecular Formula |
C₁₅H₁₁CLFN₃O₂
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| Molecular Weight |
319.72
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| Exact Mass |
319.052
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| CAS # |
184475-71-6
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| Related CAS # |
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| PubChem CID |
10471217
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
478.8±45.0 °C at 760 mmHg
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| Melting Point |
>260ºC (dec.)
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| Flash Point |
243.4±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.702
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| LogP |
3.56
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JLVTVCRXFMLUIF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11ClFN3O2/c1-22-14-6-12-9(5-13(14)21)15(19-7-18-12)20-8-2-3-11(17)10(16)4-8/h2-7,21H,1H3,(H,18,19,20)
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| Chemical Name |
4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-ol; 4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-ol
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| Synonyms |
FAAH-IN-2; O-Desmorpholinopropyl Gefitinib; JLVTVCRXFMLUIF-UHFFFAOYSA-N
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.51 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 | 3.1277 mL | 15.6387 mL | 31.2774 mL | |
| 5 mM | 0.6255 mL | 3.1277 mL | 6.2555 mL | |
| 10 mM | 0.3128 mL | 1.5639 mL | 3.1277 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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