2. Membrane Transporter/Ion Channel PI3K/Akt/mTOR NF-κB MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation Apoptosis
  3. Potassium Channel PI3K NF-κB Akt p38 MAPK ERK COX NO Synthase JNK Apoptosis
  4. Oxypeucedanin

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.

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Oxypeucedanin Chemical Structure

Oxypeucedanin Chemical Structure

CAS No. : 737-52-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Oxypeucedanin:

Oxypeucedanin Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Akt Akt1 Akt2 Akt3

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

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COX COX-1 COX-2 COX-3

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nNOS iNOS eNOS

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JNK1 JNK2 JNK3 JNK

  • Biological Activity

  • Purity & Documentation

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Description

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[1][2][3][4][5].

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.

Oxypeucedanin Related Antibodies

Cell Viability Assay[2]

Cell Line: DU145 cells
Concentration: 25, 50 and 100 μM
Incubation Time: 24, 48 and 72 h
Result: Inhibited cell growth.
Induced cell death.

Western Blot Analysis[2]

Cell Line: DU145 cells
Concentration: 25, 50 and 100 μM
Incubation Time: 24, 48 and 72 h
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.

Western Blot Analysis[3]

Cell Line: RAW264.7 cells
Concentration: 6.25 and 12.5 μM
Incubation Time: 2, 13 h
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.

RT-PCR[3]

Cell Line: RAW264.7 cells
Concentration: 6.25 and 12.5 μM
Incubation Time: 7 h
Result: Down-regulated the mRNA levels of inflammatory factors iNOS, COX-2, IL-6, IL-1β, and TNF-α.
Parmacokinetics[5]
Species Dose Route Indicator value
Rat 10 mg/kg i.v. Cmin 1662.94 μg/L
Rat 2.5 mg/kg i.v. Cmin 1140.35 μg/L
Rat 20 mg/kg i.g. Cmax 64.64 μg/L
Rat 5 mg/kg i.v. Cmin 1393.22 μg/L
Rat 10 mg/kg i.v. AUC0-t 1.28 mg·h/L
Rat 2.5 mg/kg i.v. AUC0-t 0.48 mg·h/L
Rat 20 mg/kg i.g. Tmax 3.38 hr
Rat 5 mg/kg i.v. AUC0-t 0.76 mg·h/L
Rat 10 mg/kg i.v. AUC0-∞ 1.29 mg·h/L
Rat 2.5 mg/kg i.v. AUC0-∞ 0.48 mg·h/L
Rat 20 mg/kg i.g. AUC0-t 0.28 mg·h/L
Rat 5 mg/kg i.v. AUC0-∞ 0.77 mg·h/L
Rat 10 mg/kg i.v. MRT 0.80 hr
Rat 2.5 mg/kg i.v. MRT 0.62 hr
Rat 20 mg/kg i.g. AUC0-∞ 0.32 mg·h/L
Rat 5 mg/kg i.v. MRT 0.72 hr
Rat 20 mg/kg i.g. MRT 5.86 hr
Rat 20 mg/kg i.g. F 10.26 %
In Vivo

Oxypeucedanin (10/15 mg/kg, i.p., once) inhibits lung inflammatory damage in a lipopolysaccharide (LPS)-induced acute lung injury (ALI) mouse model in a dose-dependent manner and induces the integrity of the lung air-blood barrier in mice[3].
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.

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]
Dosage: 10 and 15 mg/kg
Administration: Intraperitoneal injection (i.p.), once
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.
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]
Dosage: 13.5 mg/kg
Administration: Oral gavage (p.o.)
Result: Reduced swelling, redness and bone erosions.
Increased talus volume.
Molecular Weight

286.28

Formula

C16H14O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1(C)C(O1)COC2=C(C=CO3)C3=CC(O4)=C2C=CC4=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4931 mL 17.4654 mL 34.9308 mL
5 mM 0.6986 mL 3.4931 mL 6.9862 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 (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.

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  • 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

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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    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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (8.73 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:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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).

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

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

Purity: 99.50%

SDS (393 KB)

COA (266 KB) HNMR (248 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 (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
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Oxypeucedanin Related Classifications

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.

Keywords:

Oxypeucedanin737-52-0Potassium ChannelPI3KNF-κBAktp38 MAPKERKCOXNO SynthaseJNKApoptosisKcsAPhosphoinositide 3-kinaseNuclear factor-κBNuclear factor-kappaBPKBProtein kinase BExtracellular signal regulated kinasesCyclooxygenaseNitric oxide synthasesNOSc-Jun N-terminal kinaseanticanceranti-inflammatoryantioxidantantiarrhythmicDU145RAW264.7hKv1.5 channelLPS-induced ALI mouse modelAPDInhibitorinhibitorinhibit

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