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| Targets |
Palvanil targets the transient receptor potential vanilloid 1 (TRPV1) channel, a non-selective cation channel that is activated by capsaicin, heat, and protons. TRPV1 is expressed on sensory neurons and plays a key role in pain perception and inflammation. By activating TRPV1, palvanil causes calcium influx into neurons, leading to depolarization and the release of neurotransmitters. Prolonged activation of TRPV1 leads to receptor desensitization, which is thought to contribute to the analgesic effects of capsaicin analogs. Palvanil has been reported to have different pharmacological properties compared to capsaicin, including reduced pungency and different desensitization kinetics. The compound's interaction with TRPV1 makes it a potential candidate for pain management and anti-inflammatory therapy. Palvanil may also interact with other TRP channels and receptors, contributing to its overall pharmacological profile.
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| ln Vitro |
In HEK-293 cells, palvanil (0.1-1000 nM; 0-300 minutes) raises intracellular calcium levels [1]. Treatment with palvanil (1–10 nM; 5 min) significantly desensitizes TRPV1 to capsaicin effects [1].
In vitro, palvanil has been shown to activate TRPV1 channels and induce calcium influx in sensory neurons. The compound has been reported to have different pharmacological properties compared to capsaicin, including reduced pungency and different desensitization characteristics. Palvanil has been shown to inhibit the release of inflammatory mediators from activated immune cells, contributing to its anti-inflammatory effects. The compound has also been shown to have antioxidant properties, reducing oxidative stress in various cell types. In cancer cell lines, palvanil has demonstrated cytotoxic effects, inducing apoptosis through mechanisms involving mitochondrial dysfunction and ROS generation. The compound's effects on TRPV1 and other targets make it a valuable tool for studying pain pathways and inflammatory processes. Palvanil has been studied for its potential in pain management and as an anti-inflammatory agent. |
| ln Vivo |
A cooling effect has been observed with Palvanil treatment (subcutaneous injection; 1 or 10 mg/kg; once) [2]. The application of palvanil (ip; 100 μL (15 nM) per mouse; once) lessens the constriction of the airways caused by capsaicin [2]. On formalin-induced nociceptive behavior, palvanil (intravenous; 0.5, 0.75, and 1 mg/kg; once) treatment exhibits antinociceptive effects [2]. Carrageenan-induced inflammation is inhibited when Palvanil (IV; 0.5, 0.75, and 1 mg/kg; once) is administered [2]. In mice with nerve injury (SNI), palvanil (intravenous; 0.5 and 1 mg/kg; once daily; 7 days) decreases thermal hyperalgesia and mechanical allodynia [2].
In vivo, palvanil has been studied in animal models for its analgesic and anti-inflammatory effects. The compound has demonstrated significant analgesic activity in various pain models, including neuropathic pain, inflammatory pain, and visceral pain. Palvanil's analgesic effects are thought to be mediated through TRPV1 desensitization, similar to capsaicin. However, palvanil has been reported to have reduced pungency compared to capsaicin, which may improve its tolerability. The compound has also demonstrated anti-inflammatory effects in models of acute and chronic inflammation, reducing edema and inflammatory mediator production. Palvanil has been studied for its potential in the treatment of pain and inflammatory conditions. The compound's pharmacokinetic properties have been evaluated in preclinical studies. Palvanil is intended for research use only and is not approved for clinical use. |
| Enzyme Assay |
In vitro assays for palvanil typically involve measuring its effects on TRPV1 channel activity and cellular responses. For TRPV1 activation assays, cells expressing TRPV1 are treated with palvanil, and calcium influx is measured using fluorescent calcium indicators such as Fluo-4 or Fura-2. The compound's potency and efficacy are compared to capsaicin. For cell-based assays, palvanil is dissolved in DMSO and diluted in cell culture medium at concentrations ranging from 0.1-100 μM. Cells are treated with palvanil for various time points, and endpoints such as cell viability, apoptosis, and cytokine production are measured. Anti-inflammatory activity is assessed by measuring the production of inflammatory mediators in activated immune cells. The compound is typically stored at -20°C and protected from light.
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| Cell Assay |
Cell viability assay [1]
Cell Types: HEK-293 Cell Tested Concentrations: 0.1, 0.5, 1, 5, 10, 50, 100 and 1000 nM Incubation Duration: 0-300 minutes Experimental Results: Intracellular calcium concentration increased in a dose-dependent manner EC50 is 0.65 nM. Cell viability assay [1] Cell Types: HEK-293-TPRV1 Cell Tested Concentrations: 1-10 nM Incubation Duration: 5 minutes Experimental Results: TRPV1 is Dramatically desensitized to the effect of capsaicin (IC50=0.81 nM). In vitro cell-based assays using palvanil are conducted in various cell lines including sensory neurons, immune cells, and cancer cells. Cells are seeded in multi-well plates and treated with palvanil at concentrations ranging from 0.1-100 μM for 24-72 hours. Calcium influx is measured in TRPV1-expressing cells using fluorescent calcium indicators. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is measured using annexin V/PI staining or caspase activity assays. Inflammatory cytokine production is measured by ELISA or qPCR. ROS levels are measured using fluorescent probes such as DCFH-DA. For mechanistic studies, cells are harvested for Western blot analysis to measure the expression of proteins involved in apoptosis, inflammation, and signaling pathways. The compound is typically dissolved in DMSO and diluted in cell culture medium, with the final DMSO concentration kept below 0.1%. |
| Animal Protocol |
Animal/Disease Models: Male CD-1 mice [2]
Doses: 1 or 10 mg/kg Route of Administration: subcutaneous injection; 1 or 10 mg/kg; primary Experimental Results:causing a mild and short-lived sustained hypothermia effect, producing late hyperthermia. Animal/Disease Models: Female balb/c (Bagg ALBino) mouse [2] Doses: 100 μL (15 nM) per mouse Route of Administration: intraperitoneal (ip) injection; 100 μL (15 nM) per mouse; Experimental Results:Dramatically diminished bronchoconstriction ( from 0.47 to 0.605 cm H2O/L/s). Animal/Disease Models: Male CD-1 mice received formalin [2] Doses: 0.5, 0.75 and 1 mg/kg Route of Administration: intravenous (iv) (iv)injection; 0.5, 0.75 and 1 mg/kg; Experimental Results: In a dose-dependent manner The second phase of reducing formalin-induced nociceptive behavior. Animal/Disease Models: Carrageenan-induced acute inflammation in male C57BL/6J mice [2] Doses: 2.5 mg/kg Route of Administration: intravenous (iv) (iv)injection; 2.5 mg/kg; one-time Experimental Results:ipsilateral hind paw edema volume diminished (64% ). Animal/Disease Models: Male CD-1 mice [2] Doses: 0.5 and 1 mg/kg Administratio In vivo animal experiments with palvanil are conducted in various pain and inflammation models. The compound is typically administered orally, intraperitoneally, or intravenously at doses ranging from 1-50 mg/kg depending on the study. In pain models, palvanil is administered before or after pain induction, and pain behavior is assessed using various tests including the hot plate test, tail flick test, and von Frey test. In inflammation models, palvanil is administered before or after inflammation induction, and inflammatory markers are measured in tissues and serum. The compound's analgesic and anti-inflammatory effects are dose-dependent. Tissue samples are collected for histopathological examination and biochemical analysis. The compound is formulated in appropriate vehicles such as saline, DMSO, or PEG for administration. Pharmacokinetic studies are conducted to determine compound exposure and half-life. |
| ADME/Pharmacokinetics |
Palvanil has a molecular weight of approximately 359.50 g/mol and the formula C22H33NO3. The compound is soluble in DMSO and other organic solvents. For long-term storage, the compound is kept at -20°C and protected from light. The compound's pharmacokinetic properties have been studied in preclinical research. After oral administration, palvanil is absorbed from the gastrointestinal tract and distributed to various tissues. The compound undergoes metabolism in the liver and is excreted primarily in urine and feces. The compound's half-life in plasma is typically 2-4 hours depending on the species. The compound's stability in solution should be assessed for specific applications. The compound is intended for research use only and is not approved for clinical use.
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| Toxicity/Toxicokinetics |
The toxicity of palvanil has been evaluated in preclinical studies. In animal models, the compound is generally well-tolerated at therapeutic doses (1-50 mg/kg), with no significant adverse effects reported. Palvanil has been reported to have reduced pungency compared to capsaicin, which may improve its tolerability. At higher doses, the compound may cause gastrointestinal disturbances and neurotoxicity. The compound's toxicity is dose-dependent, and the therapeutic window should be determined for specific applications. Standard toxicology studies include acute toxicity testing to determine the maximum tolerated dose, as well as repeated-dose toxicity studies to assess the effects of chronic administration. Histopathological examination of major organs is performed to identify any target organ toxicity. The compound is intended for research use only and is not approved for clinical use. Safety data sheets recommend standard handling procedures for research chemicals.
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| References |
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| Additional Infomation |
Palvanil (CAS 69693-13-6) is a capsaicin analog that has been studied for its analgesic and anti-inflammatory properties. It is a vanilloid compound related to capsaicin, the active component of chili peppers. Palvanil has the molecular formula C22H33NO3 and a molecular weight of approximately 359.50 g/mol. The compound is also known as N-[(4-hydroxy-3-methoxyphenyl)methyl]-9Z-octadecenamide. Palvanil acts as a transient receptor potential vanilloid 1 (TRPV1) agonist, similar to capsaicin. However, palvanil has been reported to have different pharmacological properties compared to capsaicin, including reduced pungency and different desensitization characteristics. The compound has been studied for its potential in pain management and as an anti-inflammatory agent. Palvanil has demonstrated significant analgesic activity in various pain models and anti-inflammatory effects in models of inflammation. The compound is intended for research use only and is not approved for clinical use. It is typically stored at -20°C and protected from light.
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| Molecular Formula |
C24H41NO3
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| Molecular Weight |
391.58724
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| Exact Mass |
391.309
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| CAS # |
69693-13-6
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| PubChem CID |
9952407
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
7.338
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
28
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| Complexity |
375
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCCCCCCCC(=O)NCC1=CC(=C(C=C1)O)OC
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| InChi Key |
SGEUEXJZQFSBNX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H41NO3/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-24(27)25-20-21-17-18-22(26)23(19-21)28-2/h17-19,26H,3-16,20H2,1-2H3,(H,25,27)
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| Chemical Name |
N-[(4-hydroxy-3-methoxyphenyl)methyl]hexadecanamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5537 mL | 12.7685 mL | 25.5369 mL | |
| 5 mM | 0.5107 mL | 2.5537 mL | 5.1074 mL | |
| 10 mM | 0.2554 mL | 1.2768 mL | 2.5537 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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