1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. Palvanil

Palvanil is a Capsaicin (HY-10448) analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects.

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Palvanil

Palvanil Chemical Structure

CAS No. : 69693-13-6

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Description

Palvanil is a Capsaicin (HY-10448) analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects[1][2].

Cellular Effect
Cell Line Type Value Description References
EFM-19 IC50
1 μM
Compound: 3
Antiproliferative activity in human EFM-19 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity in human EFM-19 cells assessed as cell growth inhibition by MTT assay
[PMID: 33508189]
MCF7 IC50
2.2 μM
Compound: 3
Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition by MTT assay
[PMID: 33508189]
T47D IC50
1.6 μM
Compound: 3
Antiproliferative activity in human T47D cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity in human T47D cells assessed as cell growth inhibition by MTT assay
[PMID: 33508189]
In Vitro

Palvanil (0.1-1000 nM; 0-300 min) leads to calcium increasment in HEK-293 intracellular[1].
Palvanil (1-10 nM; 5 min) treatment desensitizes TRPV1 to the effect of Capsaicin significantly[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HEK-293 cells
Concentration: 0.1, 0.5, 1, 5, 10, 50, 100 and 1000 nM
Incubation Time: 0-300 min
Result: Produced a dose-dependent increase in intracellular calcium with a EC50 of 0.65 nM.

Cell Viability Assay[1]

Cell Line: HEK-293-TPRV1 cells
Concentration: 1-10 nM
Incubation Time: 5 min
Result: Desensitized TRPV1 to the effect of Capsaicin significantly (IC50=0.81 nM).
In Vivo

Palvanil (subcutaneous injection; 1 or 10 mg/kg; once) treatment shows hypothermic effect[2].
Palvanil (intraperitoneal injection; 100 μL (15 nM) per mouse; once) treatment reduces Capsaicin-induced bronchoconstriction[2].
Palvanil (intravenous injection; 0.5, 0.75, and 1 mg/kg; once) treatment shows antinociceptive effects on Formalin-induced nocifensive behavior[2].
Palvanil (intravenous injection; 0.5, 0.75, and 1 mg/kg; once) treatment inhibits Carrageenan-induced inflammation[2].
Palvanil (intravenous injection; 0.5 and 1 mg/kg; once daily; 7 days) reduces mechanical allodynia and thermal hyperalgesia in spared nerve injury (SNI) mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD-1 mice[2]
Dosage: 1 or 10 mg/kg
Administration: Subcutaneous injection; 1 or 10 mg/kg; once
Result: Led to a slight and short lasting hypothermic effect, produced late hyperthermia.
Animal Model: Female BALB/C mice[2]
Dosage: 100 μL (15 nM) per mouse
Administration: Intraperitoneal injection; 100 μL (15 nM) per mouse; once
Result: Induced a significantly lower bronchoconstriction (from 0.47 to 0.605 cm H2O/L/s).
Animal Model: Male CD-1 mice received formalin[2]
Dosage: 0.5, 0.75, and 1 mg/kg
Administration: Intravenous injection; 0.5, 0.75, and 1 mg/kg; once
Result: Reduced the second phase of Formalin-induced nociceptive behaviour in a dose-dependent manner.
Animal Model: Male C57BL/6J mice with acute inflammation induced by Carrageenan[2]
Dosage: 2.5 mg/kg
Administration: Intravenous injection; 2.5 mg/kg; once
Result: Reduced the volume of the oedema in the ipsilateral hind paw (64%).
Animal Model: Male CD-1 mice[2]
Dosage: 0.5 and 1 mg/kg
Administration: Intravenous injection; 0.5 and 1 mg/kg; once daily; 7 days
Result: Reduced mechanical allodynia and thermal hyperalgesia at 3 and 7 days after nerve injury in a dose-dependent manner.
Molecular Weight

391.59

Formula

C24H41NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCCCCCCCCCCCCCC(NCC1=CC=C(O)C(OC)=C1)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (63.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5537 mL 12.7685 mL 25.5369 mL 63.8423 mL
5 mM 0.5107 mL 2.5537 mL 5.1074 mL 12.7685 mL
10 mM 0.2554 mL 1.2768 mL 2.5537 mL 6.3842 mL
15 mM 0.1702 mL 0.8512 mL 1.7025 mL 4.2562 mL
20 mM 0.1277 mL 0.6384 mL 1.2768 mL 3.1921 mL
25 mM 0.1021 mL 0.5107 mL 1.0215 mL 2.5537 mL
30 mM 0.0851 mL 0.4256 mL 0.8512 mL 2.1281 mL
40 mM 0.0638 mL 0.3192 mL 0.6384 mL 1.5961 mL
50 mM 0.0511 mL 0.2554 mL 0.5107 mL 1.2768 mL
60 mM 0.0426 mL 0.2128 mL 0.4256 mL 1.0640 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Palvanil
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HY-137988
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