| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PF-750 targets fatty acid amide hydrolase (FAAH), a serine hydrolase that is the primary enzyme responsible for the degradation of endocannabinoids such as anandamide (AEA). FAAH hydrolyzes anandamide to arachidonic acid and ethanolamine, thereby terminating its signaling at cannabinoid receptors. By inhibiting FAAH, PF-750 increases the levels of anandamide and other fatty acid amides in the central nervous system and periphery, enhancing endocannabinoid signaling. PF-750 is a covalent/irreversible inhibitor that forms a covalent bond with the active site serine of FAAH. The compound is selective for FAAH over other serine hydrolases, making it a valuable tool for studying the role of FAAH in the endocannabinoid system.
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| ln Vitro |
PF-750 is a novel mechanistic class of FAAH inhibitors. PF-750 show higher in vitro potencies than previously established classes of FAAH inhibitors. Rather unexpectedly based on the high chemical stability of the urea functional group, PF-750 were found to inhibit FAAH in a time-dependent manner by covalently modifying the enzyme's active site serine nucleophile. Activity-based proteomic profiling revealed that PF-750 were completely selective for FAAH relative to other mammalian serine hydrolases. We hypothesize that this remarkable specificity derives, at least in part, from FAAH's special ability to function as a C(O)-N bond hydrolase, which distinguishes it from the vast majority of metabolic serine hydrolases in mammals that are restricted to hydrolyzing esters and/or thioesters.
PF-750 demonstrates potent in vitro activity as a FAAH inhibitor. The compound is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.6 μM when preincubated with recombinant human FAAH for 5 minutes and 0.016 μM (16 nM) when preincubated for 60 minutes. The compound's IC50 values vary from 16.2 to 595 nM depending on preincubation conditions. PF-750's covalent binding mechanism ensures sustained inhibition of FAAH. The compound's potent and selective FAAH inhibition makes it a valuable tool for studying the role of FAAH in endocannabinoid signaling, pain management, neuroinflammation, and neurological disorders. |
| ln Vivo |
PF-750 has been evaluated in vivo for its effects on endocannabinoid signaling. By inhibiting FAAH, PF-750 increases the levels of anandamide and other fatty acid amides, which can modulate pain, inflammation, and neurological function. The compound is a valuable tool for studying the therapeutic potential of FAAH inhibition in pain management, neuroinflammation, and neurological disorders. Detailed in vivo efficacy data, including specific model results and dosing regimens, are available in the primary literature. PF-750 is a valuable tool for validating FAAH as a therapeutic target.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for PF-750 measures the inhibition of FAAH enzymatic activity. Recombinant human FAAH enzyme is incubated with varying concentrations of PF-750 (typically ranging from nanomolar to micromolar) in the presence of a fluorescent or radiolabeled FAAH substrate (e.g., anandamide or arachidonoyl-7-amino-4-methylcoumarin amide). Preincubation times may vary (5 or 60 minutes) to assess time-dependent inhibition. The enzymatic reaction is monitored by measuring the hydrolysis of the substrate. IC50 values are determined by fitting dose-response curves to the inhibition data (0.6 μM at 5 min preincubation, 0.016 μM at 60 min preincubation). The compound is dissolved in DMSO and diluted in assay buffer. Selectivity is assessed by testing the compound against other serine hydrolases. Appropriate positive controls and negative controls are included in each assay run.
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| Cell Assay |
The in vitro cellular assay for PF-750 is performed using cells that express FAAH, such as neuronal cells, macrophages, or FAAH-transfected cell lines. Cells are cultured in appropriate medium and treated with varying concentrations of PF-750 or vehicle control (DMSO) for specified time points. Following treatment, cells are lysed and FAAH activity is measured using a fluorescent or radiolabeled substrate. The inhibition of FAAH activity is quantified, and IC50 values are determined. Additionally, the levels of anandamide and other fatty acid amides in cell lysates or culture medium can be measured by LC-MS to confirm FAAH inhibition. The compound's effects on downstream signaling pathways (e.g., cannabinoid receptor signaling) can also be assessed.
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| Animal Protocol |
In vivo animal experiments with PF-750 are conducted using rodent models of pain, inflammation, or neurological disorders. PF-750 is administered via intraperitoneal or subcutaneous injection at various doses. Endocannabinoid levels (e.g., anandamide, 2-AG) in brain and peripheral tissues are measured by LC-MS to confirm FAAH inhibition. Pain responses are assessed using models such as the formalin test, hot plate test, or neuropathic pain models. Inflammatory markers and neurological endpoints are measured as appropriate. The compound's effects on pain, inflammation, and neurological function are compared to vehicle-treated controls. Detailed experimental protocols are described in the primary literature.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) parameters for PF-750 are not extensively documented in publicly available sources. The compound has a molecular weight of 337.42 (free base) and a chemical formula of C22H23N3O. PF-750 is soluble in DMSO for formulation purposes. For in vivo administration, the compound is typically formulated using appropriate vehicles to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are available in the primary literature and should be consulted for specific experimental planning.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for PF-750 are not extensively documented in publicly available sources. As a research-grade compound, PF-750 is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound should be stored according to the manufacturer's recommendations to maintain stability and prevent degradation. Comprehensive toxicological profiling (e.g., LD50, maximum tolerated dose, organ-specific toxicity) is not available from the current search results and would require consultation of the primary literature or safety data sheets.
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| References | |
| Additional Infomation |
N-Phenylacetyl-4-(3-quinolinylmethyl)-1-piperidinecarboxamide is a member of the quinoline class of compounds.
PF-750 is a research compound developed for studying the role of FAAH in the endocannabinoid system and for evaluating FAAH inhibition as a therapeutic strategy for pain management, neuroinflammation, and neurological disorders. The compound is a potent, selective, and covalent/irreversible FAAH inhibitor with IC50 values of 0.6 μM (5 min preincubation) and 0.016 μM (60 min preincubation). PF-750's covalent binding mechanism ensures sustained inhibition of FAAH. PF-750 is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical pharmacology research. PF-750 is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C22H23N3O
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|---|---|
| Molecular Weight |
345.43800
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| Exact Mass |
345.184
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| CAS # |
959151-50-9
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| PubChem CID |
25154868
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
582.7±32.0 °C at 760 mmHg
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| Flash Point |
306.2±25.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.672
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| LogP |
3.77
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
454
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BIODYGOZWZNCAG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23N3O/c26-22(24-20-7-2-1-3-8-20)25-12-10-17(11-13-25)14-18-15-19-6-4-5-9-21(19)23-16-18/h1-9,15-17H,10-14H2,(H,24,26)
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| Chemical Name |
1-Piperidinecarboxamide, N-phenyl-4-(3-quinolinylmethyl)-
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| Synonyms |
PF-750; PF 750; PF750.
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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 |
| 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 : ~100 mg/mL (~289.49 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8949 mL | 14.4743 mL | 28.9486 mL | |
| 5 mM | 0.5790 mL | 2.8949 mL | 5.7897 mL | |
| 10 mM | 0.2895 mL | 1.4474 mL | 2.8949 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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