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Palvanil

Cat No.:V43612 Purity: ≥98%
Palvanil is a Capsaicin analog that displays strong desensitization ability to TRPV1 receptors and has anti-pain and anti~inflammatory effects.
Palvanil
Palvanil Chemical Structure CAS No.: 69693-13-6
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
Other Sizes
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Product Description
Palvanil is a Capsaicin analog that displays strong desensitization ability to TRPV1 receptors and has anti-pain and anti~inflammatory effects.
Biological Activity I Assay Protocols (From Reference)
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].
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].
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).
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
References

[1]. N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and anti-hyperalgesic activity. Pharmacol Res. 2011 Apr;63(4):294-9.

[2]. Palvanil, a non-pungent capsaicin analogue, inhibits inflammatory and neuropathic pain with little effects on bronchopulmonary function and body temperature. Pharmacol Res. 2012 Sep;66(3):243-50.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H41NO3
Molecular Weight
391.58724
Exact Mass
391.309
CAS #
69693-13-6
PubChem CID
9952407
Appearance
Typically exists as solid at room temperature
LogP
7.338
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
17
Heavy Atom Count
28
Complexity
375
Defined Atom Stereocenter Count
0
SMILES
CCCCCCCCCCCCCCCC(=O)NCC1=CC(=C(C=C1)O)OC
InChi Key
SGEUEXJZQFSBNX-UHFFFAOYSA-N
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)
Chemical Name
N-[(4-hydroxy-3-methoxyphenyl)methyl]hexadecanamide
HS Tariff Code
2934.99.9001
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)
Solubility Data
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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