1. Neuronal Signaling NF-κB Immunology/Inflammation Metabolic Enzyme/Protease MAPK/ERK Pathway
  2. Cholinesterase (ChE) NF-κB NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species Nuclear Factor of activated T Cells (NFAT) p38 MAPK
  3. Pteryxin

Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC50=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca2+-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease.

For research use only. We do not sell to patients.

Pteryxin Chemical Structure

Pteryxin Chemical Structure

CAS No. : 13161-75-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Pteryxin

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC50=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca2+-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease[1][2][3][4][5].

IC50 & Target[5]

BChE

12.96 μg/mL (IC50)

AChE

 

NLRP3

 

NFATc1

 

Nrf2-ARE

 

In Vitro

MTT cell viability assay:
Pteryxin (5-20 μM; 24 h) has no significant toxicity to RAW264.7 macrophages and BMMs osteoclast precursor cells[1][2].
ELISA inflammatory factor detection:
IL-6 and TNF-α in RAW264.7 cells[1].
WB protein analysis:
Pteryxin (5-20 μM; 24 h) concentration-dependently downregulates the expression of iNOS, COX-2, p-p38/p-ERK/p-JNK, p-p65 and NLRP3/ASC/Caspase-1 p20 proteins in RAW264.7 cells, and inhibits the expression of NFATc1/c-FOS/CTSK proteins in BMMs cells[1][2].
IF immunofluorescence:
Pteryxin (20 μM; 24 h) blocks NF-κB p65 nuclear translocation and NLRP3/ASC speck formation in RAW264.7 cells, and reduces F-actin ring area and NFATc1 nuclear localization in BMMs cells[1][2].
qPCR gene expression:
Pteryxin (5-20 μM; 24 h) upregulates antioxidant genes such as HO-1, GCLC, and Trxr1 in MIN6 islet cells, and downregulates Acp5/Mmp9/Dc-stamp[2][3] in BMMs cells[2][3].

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

Cell Viability Assay[2]

Cell Line: BMMs (bone marrow-derived macrophages)
Concentration: 5, 10, 15, 20, 25 μM
Incubation Time: 48-96 h
Result: Resulted viability >85% at ≤20 μM, while reduced viability by 12% at 25 μM for 96 h, confirming safety for osteoclastogenesis assays.
In Vivo

Acute lung injury (ALI) model:
Pteryxin (5/10 mg/kg; intraperitoneal injection; once a day; 3 days) significantly attenuates LPS (5 mg/kg, i.t.)-induced lung inflammation in C57BL/6 mice, reduces lung wet/dry weight ratio, myeloperoxidase (MPO) activity, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and IL-6/TNF-α levels[1].
Osteoporosis (OVX) model:
Pteryxin (10 mg/kg; oral; once a day; 8 weeks) significantly inhibits bone loss in ovariectomized C57BL/6 female mice, increases bone mineral density and trabecular number, reduces osteoclast number, and downregulates serum TRACP-5b and CTX-1 levels[2].
Diabetic nephropathy (DN) model:

Pteryxin (20 mg/kg; gavage; once daily; 12 weeks) improves STZ-induced renal function in db/db mice, reduced urine protein, serum creatinine and urea nitrogen, alleviates glomerular mesangial proliferation and fibrosis, and inhibits renal NF-κB activation and TGF-β1 expression[3].

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

Animal Model: C57BL/6 mice (male, 20-22 g, 8 weeks old), LPS (5 mg/kg, i.t.)-induced ALI[1]
Dosage: 5 or 10 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 3 days (starting 1 h prior to LPS).
Result: Decreased lung wet/dry ratio from 5.8±0.3 (LPS group) to 4.3±0.2 (10 mg/kg); reduced MPO activity from 2.5±0.2 U/mg to 1.4±0.1 U/mg, BALF total cells from 1.2×106±0.1×106 to 0.5×106±0.05×106, IL-6 from 850±60 pg/mL to 320±30 pg/mL, TNF-α from 520±40 pg/mL to 210±20 pg/mL.
Molecular Weight

386.40

Formula

C21H22O7

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C/C=C(C)\C(O[C@@H]1C2=C3C(C=CC(O3)=O)=CC=C2OC(C)(C)[C@@H]1OC(C)=O)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (258.80 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 2.5880 mL 12.9400 mL 25.8799 mL
5 mM 0.5176 mL 2.5880 mL 5.1760 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (6.47 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

Animal weight
(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:
%
DMSO +
+
%
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5880 mL 12.9400 mL 25.8799 mL 64.6998 mL
5 mM 0.5176 mL 2.5880 mL 5.1760 mL 12.9400 mL
10 mM 0.2588 mL 1.2940 mL 2.5880 mL 6.4700 mL
15 mM 0.1725 mL 0.8627 mL 1.7253 mL 4.3133 mL
20 mM 0.1294 mL 0.6470 mL 1.2940 mL 3.2350 mL
25 mM 0.1035 mL 0.5176 mL 1.0352 mL 2.5880 mL
30 mM 0.0863 mL 0.4313 mL 0.8627 mL 2.1567 mL
40 mM 0.0647 mL 0.3235 mL 0.6470 mL 1.6175 mL
50 mM 0.0518 mL 0.2588 mL 0.5176 mL 1.2940 mL
60 mM 0.0431 mL 0.2157 mL 0.4313 mL 1.0783 mL
80 mM 0.0323 mL 0.1617 mL 0.3235 mL 0.8087 mL
100 mM 0.0259 mL 0.1294 mL 0.2588 mL 0.6470 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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