Oxypeucedanin
Based on 1 Customer Validation
Oxypeucedanin is a furanocoumarin derivative found in Angelica dahurica. Oxypeucedanin is an orally active PI3K/AKT/NF-κB, MAPK, and ROS inhibitor. Oxypeucedanin induces cell cycle arrest and apoptosis. Oxypeucedanin inhibits hKv1.5 channel currents (IC50: 76 nM). Oxypeucedanin exhibits anticancer, anti-inflammatory, antioxidant and antiarrhythmic activities.
For research use only. We do not sell to patients.
- Purity : 99.50%
- CAS No.: 737-52-0
- Formula: C16H14O5
- Molecular Weight:286.28
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
IC50: HKv1.5 current; apoptosis[1]
In Vitro
oxypeucedanin (1-1000 nM) inhibits hKv1.5 channel currents expressed in the mouse Ltk- cell lines in a concentration-dependent manner (IC50: 76 nM)[1].
oxypeucedanin (0.1-1 μM) prolongs the action potential duration (APD) of rat atrial and ventricular myocytes in a concentration-dependent manner[1].
Oxypeucedanin (25-100 μM, 24-72 h) inhibits the viability of human prostate cancer DU145 cells and induces apoptosis in a time- and dose-dependent manner[2].
Oxypeucedanin (25-100 μM, 24-48 h) induces G2-M arrest in DU145 cell cycle progression in a dose-dependent manner[2].
Oxypeucedanin (6.25-12.5 μM, 7-13 h) inhibits the expression of inflammatory factors IL-6, IL-1β, TNF-α, iNOS, COX-2 and the production of ROS in RAW264.7 cells[3].
Oxypeucedanin (6.25-12.5 μM, 2 h) inhibits the PI3K/AKT/NF-κB and MAPK signaling pathways in RAW264.7 cells[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:DU145 cells
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Concentration:25, 50 and 100 μM
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Incubation Time:24, 48 and 72 h
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Result:Inhibited cell growth.
Induced cell death.
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Cell Line:DU145 cells
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Concentration:25, 50 and 100 μM
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Incubation Time:24, 48 and 72 h
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Result:Decreased the protein levels of Cdc-25C, Cyclin A, Cyclin B1 and Cdc-2.
Increased the protein levels of Chk1, Chk2, cleaved caspase-3 and cleaved PARP.
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Cell Line:RAW264.7 cells
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Concentration:6.25 and 12.5 μM
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Incubation Time:2, 13 h
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Result:Decreased the protein levels of iNOS and COX-2.
Inhibited the phosphorylation levels of AKT, P65, P38, ERK1/2 and JNK proteins and the ubiquitination degradation of IκB proteins.
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Cell Line:RAW264.7 cells
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Concentration:6.25 and 12.5 μM
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Incubation Time:7 h
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Result:Down-regulated the mRNA levels of inflammatory factors iNOS, COX-2, IL-6, IL-1β, and TNF-α.
Parmacokinetics
| Species | Dose | Route | Plasma Concentration | AUC | MRT | Tmax | Bioavailability |
|---|---|---|---|---|---|---|---|
| Rat[5] | 10 mg/kg | i.v. | 1662.94 μg/L | 1.28 mg·h/L | 0.80 h | / | / |
| Rat[5] | 2.5 mg/kg | i.v. | 1140.35 μg/L | 0.48 mg·h/L | 0.62 h | / | / |
| Rat[5] | 20 mg/kg | i.g. | 64.64 μg/L | 0.28 mg·h/L | 5.86 h | 3.38 h | 10.26 % |
| Rat[5] | 5 mg/kg | i.v. | 1393.22 μg/L | 0.76 mg·h/L | 0.72 h | / | / |
In Vivo
Oxypeucedanin (13.5 mg/kg, p.o.) alleviates the severity of collagen-induced arthritis (CIA) model in rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced ALI mouse model (75 male BALB/c mice, ages 6-8 weeks and weights of 20-25 g; unilateral nostril drops were added to the 50 μg LPS solution to establish the ALI model)[3]
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Dosage:10 and 15 mg/kg
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Administration:Intraperitoneal injection (i.p.), once
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Result:Reduced lung pathological tissue damage.
Down-regulated the mRNA levels of inflammatory factors iNOS, COX-2, IL-6, IL-1β, and TNF-α.
Increased the protein levels of Occludin and Claudin 3.
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Animal Model:Rat CIA model (Male Wistar rats, subcutaneously injected with 200/100 μL emulsion that contained 2 mg/mL chicken type II collagen (HY-NP113) and complete/incomplete Freund’s adjuvant)[4]
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Dosage:13.5 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Reduced swelling, redness and bone erosions.
Increased talus volume.
Chemical Information
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CAS No. 737-52-0
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Appearance Solid
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Molecular Weight 286.28
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Formula C16H14O5
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Color White to off-white
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SMILES
CC1(C)C(O1)COC2=C(C=CO3)C3=CC(O4)=C2C=CC4=O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 12.5 mg/mL (43.66 mM; ultrasonic and warming and heat to 60°C; 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, 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (8.73 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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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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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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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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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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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
Purity & Documentation
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Data Sheet (297 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)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Eun JS, et al. Effects of oxypeucedanin on hKv1.5 and action potential duration. Biol Pharm Bull. 2005 Apr;28(4):657-60. [Content Brief]
[2]. Kang TJ, et al. Anti-tumor activity of oxypeucedanin from Ostericum koreanum against human prostate carcinoma DU145 cells. Acta Oncol. 2009;48(6):895-900. [Content Brief]
[3]. Du L, et al. Oxypeucedanin relieves LPS-induced acute lung injury by inhibiting the inflammation and maintaining the integrity of the lung air-blood barrier. Aging (Albany NY). 2022 Aug 18;14(16):6626-6641. [Content Brief]
[4]. Liu M, et al. Oxypeucedanin hydrate alleviates rheumatoid arthritis by inhibiting the TLR4-MD2/NF-κB/MAPK signaling axis. Acta Biochim Biophys Sin (Shanghai). 2024 May 11;56(12):1789-1801. [Content Brief]
[5]. Zheng MC, et al. Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration. Molecules. 2022 Jun 2;27(11):3570. [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, 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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4931 mL | 17.4654 mL | 34.9308 mL | 87.3271 mL |
| 5 mM | 0.6986 mL | 3.4931 mL | 6.9862 mL | 17.4654 mL | |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.4931 mL | 8.7327 mL | |
| 15 mM | 0.2329 mL | 1.1644 mL | 2.3287 mL | 5.8218 mL | |
| 20 mM | 0.1747 mL | 0.8733 mL | 1.7465 mL | 4.3664 mL | |
| 25 mM | 0.1397 mL | 0.6986 mL | 1.3972 mL | 3.4931 mL | |
| 30 mM | 0.1164 mL | 0.5822 mL | 1.1644 mL | 2.9109 mL | |
| 40 mM | 0.0873 mL | 0.4366 mL | 0.8733 mL | 2.1832 mL |
Oxypeucedanin Related Classifications
HY-N0747 Related Classifications
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