Pteryxin
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.55%
- CAS. Nr.: 13161-75-6
- Formel: C21H22O7
- Molecular Weight:386.40
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Pteryxin
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Biologische Aktivität
Beschreibung
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. Further protocols information, click here.
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Cell Line:BMMs (bone marrow-derived macrophages)
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Concentration:5, 10, 15, 20, 25 μM
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Incubation Time:48-96 h
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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
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.
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Animal Model:C57BL/6 mice (male, 20-22 g, 8 weeks old), LPS (5 mg/kg, i.t.)-induced ALI[1]
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Dosage:5 or 10 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 3 days (starting 1 h prior to LPS).
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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.
Chemical Information
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CAS. Nr. 13161-75-6
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Appearance Solid
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Molecular Weight 386.40
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Formel C21H22O7
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Color White to off-white
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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
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Synonyms
(+)-Pteryxin
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
Pteryxin suppresses osteoclastogenesis and prevents bone loss via inhibiting the MAPK/Ca2+ signaling pathways mediated by ROS. [Abstract]2023 Sep:165:114898. PMID: 37352699
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
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Osteoclast differentiation from monocyte/macrophage precursors
Osteoclast differentiation is an in vitro induction assay in which monocyte/macrophage-lineage precursors are exposed to macrophage colony-stimulating factor (M-CSF) and receptor activator of NF-κB ligand (RANKL), generating multinucleated osteoclasts that are commonly identified by tartrate-resistant acid phosphatase (TRAP) staining and functionally confirmed by resorption pits on dentin, bone, or mineralized substrates. M-CSF supports survival and expansion of osteoclast precursors, while RANKL binding to RANK drives osteoclast commitment, fusion, maturation, and resorptive function; osteoprotegerin inhibits this pathway by binding RANKL and preventing RANK activation. The main readouts are the number of TRAP-positive multinucleated cells, formation of F-actin rings, and resorbed surface area; TRAP-positive multinucleated cells indicate osteoclast differentiation, whereas pit formation on dentin, bone, or mineralized coating indicates functional bone-resorbing activity.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Reinheit & Dokumentation
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Data Sheet (288 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Zhen D, et al. Pteryxin attenuates LPS-induced inflammatory responses and inhibits NLRP3 inflammasome activation in RAW264.7 cells. J Ethnopharmacol. 2022 Feb 10;284:114753. [Content Brief]
[2]. Sun R, et al. Pteryxin suppresses osteoclastogenesis and prevents bone loss via inhibiting the MAPK/Ca2+ signaling pathways mediated by ROS. Biomed Pharmacother. 2023 Sep;165:114898. [Content Brief]
[3]. Taira J, et al. Cytoprotective Effect of Pteryxin on Insulinoma MIN6 Cells Due to Antioxidant Enzymes Expression via Nrf2/ARE Activation. Antioxidants (Basel). 2023 Mar 10;12(3):693. [Content Brief]
[4]. Kiris I, et al. Molecular Effects of Pteryxin and Scopoletin in the 5xFAD Alzheimer's Disease Mouse Model. Curr Med Chem. 2022;29(16):2937-2950. [Content Brief]
[5]. Orhan IE, et al. Pteryxin - A promising butyrylcholinesterase-inhibiting coumarin derivative from Mutellina purpurea. Food Chem Toxicol. 2017 Nov;109(Pt 2):970-974. [Content Brief]
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 |
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| 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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