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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.
For research use only. We do not sell to patients.
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[1][2][3][4][5][6][7][8].
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 acidA (GABAA) 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.
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.
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.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Solvent & Solubility
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)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
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
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
*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.
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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