Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis MAPK/ERK Pathway Stem Cell/Wnt Others Anti-infection
TRP Channel Amyloid-β Toll-like Receptor (TLR) Keap1-Nrf2 Heme Oxygenase (HO) Dihydroorotate Dehydrogenase Ferroptosis PAI-1 NF-κB ERK Proton Pump Glutathione Peroxidase Thrombin Insecticide Bacterial
Pellitorine

Cat. No.: HY-N3097

Pellitorine

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Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 98.30%
CAS No.: 18836-52-7
Formule: C₁₄H₂₅NO
Masse moléculaire:223.35

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Pellitorine Chemical Structure

CAS No.: 18836-52-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[4]^[6]

GPX4

ERK1

ERK2

TLR4

NF-κB

HO-1

Voir tous les produits spécifiques à Isoform TRP Channel :

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR) :

Voir tous les produits spécifiques à Isoform Heme Oxygenase (HO) :

HO-1
HO-2

Voir tous les produits spécifiques à Isoform NF-κB :

Voir tous les produits spécifiques à Isoform ERK :

Voir tous les produits spécifiques à Isoform Glutathione Peroxidase :

GPX1
GPX4

Cellular Effect

Cell Line	Type	Value	Description	References
BV-2	IC₅₀	45 μM Compound: 23	Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 20 hrs by Griess assay Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 20 hrs by Griess assay	[PMID: 33822610]
Hepatocyte	IC₅₀	9.3 μM Compound: 30	Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine-induced cytotoxicity after 44 hrs by MTT assay Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine-induced cytotoxicity after 44 hrs by MTT assay	[PMID: 19775895]
THP-1	IC₅₀	13.5 μg/mL Compound: 7	Inhibition of sICAM1/LFA1 interaction-mediated human THP1 cell adhesion after 1 hr by ELISA Inhibition of sICAM1/LFA1 interaction-mediated human THP1 cell adhesion after 1 hr by ELISA	[PMID: 18672369]
WI-38	IC₅₀	0.67 μM Compound: 6	Induction of senescence in human WI-38 cells Induction of senescence in human WI-38 cells	[PMID: 38436272]

In Vitro

Pellitorine exhibits cytotoxic against HL60 and MCF-7 with IC₅₀ values of 13.0 µg/mL and 1.8 µg/mL^[1].
Pellitorine (0.01-1 mg/mL) blocks Capsaicin-evoked Ca²⁺ uptake with an IC₅₀ of 154 µg/mL (0.69 mM/L) in HaCaT cells^[2].
Pellitorine (0.1 nM-100 µM) significantly prolongs partial thromboplastin time (aPTT) and prothrombin time (PT) and inhibits the activities of cell-based thrombin and activated factor X (FXa) in normal human plasma^[5].
Pellitorine (0-20 µM) Inhibits the production of thrombin and FXa induced by TNF-α and down-regulates the secretion of PAI-1, reduces the PAI-1/t-PA ratio to improve the fibrinolytic balance in HUVECs^[5].
Pellitorine (0-20 μM, 6-30 h) inhibits LPS (HY-D1056)-induced barrier disruption, expression of cell adhesion molecules (CAMs) and adhesion/transendothelial migration of monocytes to human endothelial cells^[6].
Pellitorine (0-20 μM, 7-22 h) suppresses the production of TNF-α or IL-6 and activation of NF-κB or extracellular regulated kinases (ERK) 1/2 by LPS in HUVECs^[6].
Pellitorine is active against Bacillus subtilis, Bacillus sphaericus, Staphylococcus aureus, Klebsiella aerogenes and Chromobacterium violaceum with MIC values of 28, 56, 56, 56 and 56 μM^[7].

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

Cell Migration Assay ^[6]

Cell Line:

Monocytes through HUVEC monolayers
Concentration:

0, 3, 5, 10, 20 μM
Incubation Time:

6 h
Result:

Inhibited the migration of monocytes across the endothelium.

ELISA Assay^[6]

Cell Line:

HUVECs
Concentration:

0, 3, 5, 10, 20 μM
Incubation Time:

Incubated for 6 h followed by LPS for 3 h (TLR4 and p-p38), 16 h (VCAM-1, ICAM-1, TNF-α and IL-6) or 24 h (E-Selectin)
Result:

Inhibited expression of TLR4 and p-p38 level.
Decreased VCAM-1, ICAM-1 and E-selectin.
Decreased TNF-α and IL-6.
Inhibited phosphorylation of ERK1/2 and NF-κB expression.

RT-PCR^[6]

Cell Line:

Monocytes through HUVEC monolayers
Concentration:

0, 3, 5, 10, 20 μM
Incubation Time:

6 h
Result:

Significantly inhibited the upregulation of TLR4 induced by LPS.
Decreased VCAM-1, ICAM-1 and E-selectin mRNA.

Immunofluorescence^[6]

Cell Line:

HUVECs
Concentration:

0, 3, 5, 10, 20 μM
Incubation Time:

Incubated for 6 h followed by LPS for 1 h
Result:

Reduced the nuclear translocation of NF-κB p65.

In Vivo

Pellitorine (3.75 mM with 100 µM Capsaicin, eye drops, single dose) inhibits the pain-evoked defensive movements of mice in response to pungent vanilloids^[2].
Pellitorine (2.21-5 mg/L, suspended in distilled water with Triton X-100, put Ae. Aegypti into paper cups containing the test solution) led to the collapse of the larva's osmotic pressure and its subsequent death by attacking mainly on midgut epithelium and anal gills of Aedes aegypt^[3].
Pellitorine (0.1-0.6 mg/kg, i.p., once daily for 21 days) protects chronic restraint stress (CRS)-induced cognitive deficits via inhibiting neural inflammation and ferroptosis in mice^[4].
Pellitorine (4.5-9 μg/mouse, i.v., single dose) significantly prolongs mice tail bleeding times^[5].
Pellitorine (9 μg/mouse, i.v., single or doule doses) prevents mice or results in reduction of mice mortality in the LPS-induced lethal endotoxemia model^[6].

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

Animal Model:

Eye wipe test established in BALB/c mice^[2]
Dosage:

3.75 mM applied together with 100 µM Capsaicin
Administration:

Eye drops, single dose
Result:

Significantly decreased the frequency of vanilloid-evoked defending movements.
Did not change significantly following either a 1 h or 15 min pretreatment with 3.75mM or 4.5 mM alone.

Animal Model:

Insecticide test established in insecticide-susceptible Ae. Aegypti^[3]
Dosage:

2.21 and 5 mg/L, suspended in distilled water with Triton X-100 (20 ml/L)
Administration:

Put Ae. Aegypti into paper cups containing the test solution
Result:

Caused the epithelial cells of the gastric caeca to swell, disintegrate, and the cell nuclei to fragment.
Dissolved the electron-dense substances in the epithelial cells and leaves the residual peritubular membrane.
Damaged the anal-gill structure, resulting in neuronal damage.
Inhibited AaAQP4 expression levels and disturbed the Na⁺, Cl^-, and K⁺ co-transport system mainly.
Caused the histopathological alterations and inhibition of gene expression of V-type H⁺-ATPase and aquaporin protein in the anal gills.

Animal Model:

CRS model established in seven-week-old male C57BL/6 J mice^[4]
Dosage:

0.1 and 0.6 mg/kg
Administration:

Intraperitoneally injection (i.p.), once daily for 21 days
Result:

Significantly reduced the resting time of CRS mice in tails suspension test (TST).
Improved spatial memory of mice in novel object recognition test (NOR) and morris water maze (MWM).
Suppressed ferroptosis-associated signaling pathways and neuroinflammation.
Upregulated the expressions of GPX4, DHODH and FSP1.
Prevented neuronal loss, preserved the expression of neuroprotective molecules such as BDNF, Nrf2, HO-1, phosphorylated-CREB, and phosphorylated-ERK1/2.
Reduced the protein levels of inflammation-related markers including NLRP3, HMGB1, and NF-κB.
Reduced the number of activated microglia, as indicated by decreased Iba-1⁺, TREM2⁺, CD86⁺, and CX3CR1⁺ cell populations in the hippocampus.
Did not exhibit neurotoxicity in healthy mice.

Animal Model:

Bleeding time test established in ICR mice^[5]
Dosage:

4.5 and 9 μg/mouse
Administration:

Intravenous administration (i.v.), single dose
Result:

Prolonged tail bleeding times from 41.6 s to 57.6 s and 71.8 s, respectively.

Animal Model:

LPS-induced lethal endotoxemia model established in male C57BL/6 mice^[6]
Dosage:

9 μg/mouse
Administration:

Intravenous administration (i.v.), two times at 12 h and 50 h after LPS injection or single dose at 12 h before LPS injection
Result:

Prevented LPS-induced lethal endotoxemia.
Resulted in an increase in the survival rate from 0 to 30% by Kaplan-Meier survival analysis.
Suppressed LPS-induced hyperpermeability and leukocyte migration.

Chemical Information

CAS No. 18836-52-7
Appearance Solid
Masse moléculaire 223.35
Formule C₁₄H₂₅NO
Color White to off-white
SMILES

CC(C)CNC(/C=C/C=C/CCCCC)=O
Structure Classification
- Alkaloids
- Other Alkaloids
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (223.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.4773 mL

22.3864 mL

44.7728 mL

5 mM

0.8955 mL

4.4773 mL

8.9546 mL

10 mM

0.4477 mL

2.2386 mL

4.4773 mL

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (11.19 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. Ee GC, et al. Pellitorine, a potential anti-cancer lead compound against HL6 and MCT-7 cell lines and microbial transformation of piperine from Piper Nigrum. Molecules. 2010;15(4):2398-2404. [Content Brief]

[2]. Oláh Z, et al. Pellitorine, an extract of Tetradium daniellii, is an antagonist of the ion channel TRPV1. Phytomedicine. 2017 Oct 15;34:44-49. [Content Brief]

[3]. Perumalsamy H, et al. Novel histopathological and molecular effects of natural compound pellitorine on larval midgut epithelium and anal gills of Aedes aegypti. PLoS One. 2013 Nov 18;8(11):e80226. [Content Brief]

[4]. Zhang JB, et al. Pellitorine protects chronic restraint stress-induced cognitive deficits via inhibiting neural inflammation and ferroptosis. Int Immunopharmacol. 2025 Sep 23;162:115166. [Content Brief]

[5]. Ku SK, et al. Antithrombotic activities of pellitorine in vitro and in vivo. Fitoterapia. 2013 Dec;91:1-8. doi: 10.1016/j.fitote.2013.08.004. Epub 2013 Aug 22. [Content Brief]

[6]. Lee W, et al. Vascular barrier protective effects of pellitorine in LPS-induced inflammation in vitro and in vivo. Fitoterapia. 2014 Jan;92:177-87. [Content Brief]

[7]. Reddy SV, et al. Antibacterial constituents from the berries of Piper nigrum. Phytomedicine. 2004 Nov;11(7-8):697-700. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.4773 mL	22.3864 mL	44.7728 mL	111.9319 mL
	5 mM	0.8955 mL	4.4773 mL	8.9546 mL	22.3864 mL
	10 mM	0.4477 mL	2.2386 mL	4.4773 mL	11.1932 mL
	15 mM	0.2985 mL	1.4924 mL	2.9849 mL	7.4621 mL
	20 mM	0.2239 mL	1.1193 mL	2.2386 mL	5.5966 mL
	25 mM	0.1791 mL	0.8955 mL	1.7909 mL	4.4773 mL
	30 mM	0.1492 mL	0.7462 mL	1.4924 mL	3.7311 mL
	40 mM	0.1119 mL	0.5597 mL	1.1193 mL	2.7983 mL
	50 mM	0.0895 mL	0.4477 mL	0.8955 mL	2.2386 mL
	60 mM	0.0746 mL	0.3731 mL	0.7462 mL	1.8655 mL
	80 mM	0.0560 mL	0.2798 mL	0.5597 mL	1.3991 mL
	100 mM	0.0448 mL	0.2239 mL	0.4477 mL	1.1193 mL

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Pellitorine

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