PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage Cytoskeleton Stem Cell/Wnt JAK/STAT Signaling Apoptosis MAPK/ERK Pathway Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease TGF-beta/Smad Immunology/Inflammation Anti-infection
Akt Sirtuin Integrin STAT PI3K Apoptosis ERK PPAR PKC Toll-like Receptor (TLR) HIV
Phellopterin

Cat. No.: HY-N2110

Phellopterin

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Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.

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Pureté: 99.94%
CAS No.: 2543-94-4
Formule: C₁₇H₁₆O₅
Masse moléculaire:300.31

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Phellopterin Chemical Structure

CAS No.: 2543-94-4

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

Activité biologique
- Description
- IC₅₀ & Target
- 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^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]

PI3K

SIRT3

PKC

PPARγ

Akt

ERK

TLR4

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform Sirtuin :

Voir tous les produits spécifiques à Isoform Integrin :

Voir tous les produits spécifiques à Isoform STAT :

Voir tous les produits spécifiques à Isoform PI3K :

Voir tous les produits spécifiques à Isoform ERK :

Voir tous les produits spécifiques à Isoform PPAR :

Voir tous les produits spécifiques à Isoform PKC :

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

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In Vitro

Phellopterin (1-50 μM, 24 h) significantly inhibits VCAM-1 expression and Akt and PKC phosphorylation in a dose-dependent manner in TNF-α-stimulated HUVECs, and effectively prevents monocyte adhesion to TNF-α-stimulated ECs by regulating VCAM-1 expression^[1].
Phellopterin (1-25 μM, 24 h) upregulates the expression of SIRT1 and downregulates the expression of ICAM-1 in HaCaT cells, thereby reversing the proliferation inhibition caused by IFN-γ^[2].
Phellopterin (1-16 μM, 24 h) inhibits IL-4-induced activation of STAT3, which leaded to suppress the STAT3-mediated transcription of TSLP and IL-33 in HaCaT cells^[3].
Phellopterin (1-100 μg/mL, 48 h) attenuates the proliferation of ovarian cancer cells with IC₅₀s for OV90 and SKOV3 cells of 18.67 and 27.75 μg/mL^[4].
Phellopterin (25-50 μg/mL) attenuates ovarian cancer progression by inhibiting cell proliferation through modulating DNA replication, cell cycle (G0/G1), and apoptosis in OV90 cells and SKOV3 cells^[4].
Phellopterin (25 μg/mL, 48 h) inactivates CLEC5A/PI3K/AKT signaling in OV90 cells and SKOV3 cells ^[4].
Phellopterin (12.5-100 μg/mL) induces adipocyte differentiation and increases the mRNA expression of peroxisome proliferator-activated receptors γ (PPARγ)^[5].
Phellopterin (1-500 μg/mL, 72 h) reduces the HSV-1 replication by 3.01 log at the concentration of 7.81 mg/mL, and has a significant cytotoxicity towards Vero cells with CC₅₀ of 14.61 μg/mL^[6].
Phellopterin (40 min) inhibits [³H]diazepam and [³H]Ro 15-1788 binding to the benzodiazepine site of the rat brain 3,-aminobutyric acid_A (GABA_A) receptor in vitro with IC₅₀ values of 400 and 680 nM, respectively^[7].

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

Western Blot Analysis^[1]

Cell Line:

TNF-α-stimulated HUVECs
Concentration:

1, 5, 10 and 50 μM
Incubation Time:

24 h
Result:

Did not inhibit TNF-α-induced ICAM-1 expression, whereas it inhibited VCAM-1 expression from 5 μM, and completely suppressed it at 50 μM concentration.
Had no effect on ERK1/2 phosphorylation, whereas they significantly inhibited the phosphorylation of Akt and PKC in dose-dependent manner.

Immunofluorescence^[1]

Cell Line:

TNF-α-stimulated HUVECs
Concentration:

1, 5, 10 and 50 μM
Incubation Time:

24 h
Result:

Showed significant reduction of adherent cells to ECs from 4-fold to 2.5-fold.

Cell Proliferation Assay^[2]

Cell Line:

TNF-γ-stimulated HaCaT cells
Concentration:

1, 5 and 25 μM
Incubation Time:

24 h
Result:

Stimulated HaCaT cell proliferation.
Was unable to restore cell proliferation to normal levels.

Western Blot Analysis^[2]

Cell Line:

TNF-γ-stimulated HaCaT cells
Concentration:

2, 4, 8 and 16 μM
Incubation Time:

24 h
Result:

Suppressed the STAT3-mediated transcription of TSLP and IL-33.

Western Blot Analysis^[3]

Cell Line:

IL-4-stimulated HaCaT cells
Concentration:

2, 4, 8 and 16 μM
Incubation Time:

24 h
Result:

Suppressed the STAT3-mediated expression of TSLP and IL-33.

Western Blot Analysis^[4]

Cell Line:

OV90 and SKOV3 cells
Concentration:

25 μg/mL
Incubation Time:

48 h
Result:

Significantly reduced the protein levels of CLEC5A, p-PI3K, and p-AKT.
Reduced the expression of PU.1 protein.

In Vivo

Phellopterin (0.6-2.4 mg/kg, i,v., for 14 days) significantly accelerated the wound healing by downregulating ICAM-1 expression via SIRT1 in diabetic mice^[2].
Phellopterin (0.5-4.5 mg/kg, ear topically spread, twice a day for 10 days) improves the atopic dermatitis (AD)-like lesions in mice^[3].
Phellopterin (50 mg/kg, i,g., five times a week for 4 weeks) suppresses cancer growth in mice ovarian cancer xenograft model^[4].
Phellopterin (0.5-2 mg/kg, i,g., once daily for 4 weeks) significantly lowers blood sugar levels thus prevents High-fat diet/Streptozotocin (HFD/STZ) (HY-13753)-induced type Ⅱ diabetes in mice^[5].
Phellopterin (0.5-2 mg/kg, i,g.) improves the symptoms and inflammatory response of colitis-associated cancer (CAC) and inhibits the occurrence of colon cancer by inhibiting M2 polarization of macrophages and activation of the TLR4/NF-κB pathway in mice^[8].

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

Animal Model:

Streptozotocin (STZ) -induced diabetic model established in five-week-old C57BL/6J male mice^[2]
Dosage:

0.6, 1.2 and 2.4 mg/kg
Administration:

Intravenous injection (i.v.), for 14 days
Result:

Seemed to have the greatest effect on wound healing at medium dose.
Promoted diabetic wound healing by accelerating epidermic re-epithelialization.
Downregulated ICAM-1 expression via SIRT1 in mice with diabetic ulcers.

Animal Model:

Calcipotriol (MC-903) (HY-10001) induced AD like skin model established in male C57BL/6 mice around 8 to 10 weeks of age^[3]
Dosage:

0.5, 1.5 and 4.5 mg/kg
Administration:

Ear topically spread, twice a day for 10 days
Result:

The concentration at 1.5 mg/kg showed the optimal therapeutic effect.
Exhibited significant reduction in epidermal thickness and scales as well as serum IgE levels.
Decreased the infiltrated eosinophils and mast cells.
The protein levels of TSLP and IL-33 in epidermal keratinocytes were decreased.
The expression of IL-4 was remarkably elevated in the AD-like skin lesions, but not significantly changed its expression.

Animal Model:

SKOV3 cells induced ovarian cancer xenograft model established in nude mice^[4]
Dosage:

50 mg/kg
Administration:

Intragastric administration (i.g.), five times a week for 4 weeks
Result:

Attenuated cancer growth.
No significant difference in mice body weight and the histopathological changes of the liver and kidney.
Downregulated Ki67 levels in tumor.

Animal Model:

High-fat diet/Streptozotocin (HFD/STZ)-induced diabetic established in male ICR strain mice^[5]
Dosage:

0.5, 1 and 2 mg/kg
Administration:

Intragastric administration (i.g.), once daily for 4 weeks
Result:

Decreased total cholesterol from 1154.8 to 630.4 mg/dL.
Dropped triglycerides dropped from 541.6 to 346.7 mg/dL.
Observed no obvious toxic reactions and the organ coefficients were within the normal range.

Animal Model:

Azoxymethane (AOM) (HY-111375)/DSS (Dapsone) (HY-B0688) induced colitis-associated cancer (CAC) model established in C57BL/6 mice^[8]
Dosage:

0.5, 1 and 2 mg/kg
Administration:

Intragastric administration (i.g.)
Result:

Dose-dependently improved the weight loss in mice and increased the length of their colons.
Reduced the rate of tumor formation.
Increased CD4+ and CD8+, and decreased pro-inflammatory factors (IL-6, IL-1β, TNF-α).
Reduced the levels of M2-type markers (such as CD163, CD206, etc.)
Decreased the expression of TLR4 and NF-κB p65.

Chemical Information

CAS No. 2543-94-4
Appearance Solid
Masse moléculaire 300.31
Formule C₁₇H₁₆O₅
Color Off-white to light yellow
SMILES

O=C1C=CC2=C(OC)C3=C(OC=C3)C(OC/C=C(C)/C)=C2O1
Structure Classification
- Phenylpropanoids
- Coumarins
Initial Source
- Plants
- Umbelliferae
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (332.99 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

3.3299 mL

16.6495 mL

33.2989 mL

5 mM

0.6660 mL

3.3299 mL

6.6598 mL

10 mM

0.3330 mL

1.6649 mL

3.3299 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. 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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.32 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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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:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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%

Fiche technique (295 KB)
SDS (392 KB)
- English - EN (392 KB)
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- Norwegian - NO (392 KB)
- Español - ES (392 KB)
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- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Nizamutdinova IT, et al. Hesperidin, hesperidin methyl chalone and phellopterin from Poncirus trifoliata (Rutaceae) differentially regulate the expression of adhesion molecules in tumor necrosis factor-alpha-stimulated human umbilical vein endothelial cells. Int Immunopharmacol. 2008 May;8(5):670-8. [Content Brief]

[2]. Zou J, et al. Phellopterin cream exerts an anti-inflammatory effect that facilitates diabetes-associated cutaneous wound healing via SIRT1. Phytomedicine. 2022 Dec;107:154447. [Content Brief]

[3]. Guo A, Lin J, Zhong P, Chen J, Wang L, Lin X, Feng M. Phellopterin attenuates ovarian cancer proliferation and chemoresistance by inhibiting the PU.1/CLEC5A/PI3K-AKT feedback loop. Toxicol Appl Pharmacol. 2023 Oct 15;477:116691. [Content Brief]

[4]. Han HS, Jeon H, Kang SC. Phellopterin isolated from Angelica dahurica reduces blood glucose level in diabetic mice. Heliyon. 2018 Mar 19;4(3):e00577. [Content Brief]

[5]. Nakamura M, et al. Stimulation of phosphorylation of ERK and CREB by phellopterin and auraptene isolated from Citrusjunos. Nat Prod Commun. 2014 Oct;9(10):1491-4. [Content Brief]

[6]. Rajtar B, et al. Antiviral effect of compounds derived from Angelica archangelica L. on Herpes simplex virus-1 and Coxsackievirus B3 infections. Food Chem Toxicol. 2017 Nov;109(Pt 2):1026-1031. [Content Brief]

[7]. Dekermendjian K, et al. Characterisation of the furanocoumarin phellopterin as a rat brain benzodiazepine receptor partial agonist in vitro. Neurosci Lett. 1996 Nov 29;219(3):151-4. [Content Brief]

[8]. Xu X, et al. The therapeutic effect of phellopterin on colitis-associated cancer and its effects on TLR4/NF-κB pathway and macrophage M2 polarization. Cell Mol Biol (Noisy-le-grand). 2023 Dec 31;69(15):51-57. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	3.3299 mL	16.6495 mL	33.2989 mL	83.2473 mL
	5 mM	0.6660 mL	3.3299 mL	6.6598 mL	16.6495 mL
	10 mM	0.3330 mL	1.6649 mL	3.3299 mL	8.3247 mL
	15 mM	0.2220 mL	1.1100 mL	2.2199 mL	5.5498 mL
	20 mM	0.1665 mL	0.8325 mL	1.6649 mL	4.1624 mL
	25 mM	0.1332 mL	0.6660 mL	1.3320 mL	3.3299 mL
	30 mM	0.1110 mL	0.5550 mL	1.1100 mL	2.7749 mL
	40 mM	0.0832 mL	0.4162 mL	0.8325 mL	2.0812 mL
	50 mM	0.0666 mL	0.3330 mL	0.6660 mL	1.6649 mL
	60 mM	0.0555 mL	0.2775 mL	0.5550 mL	1.3875 mL
	80 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0406 mL
	100 mM	0.0333 mL	0.1665 mL	0.3330 mL	0.8325 mL

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Phellopterin

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