1. Immunology/Inflammation
  2. PGE synthase
  3. MF63

MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1.

For research use only. We do not sell to patients.

MF63 Chemical Structure

MF63 Chemical Structure

CAS No. : 892549-43-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 100 In-stock
10 mg USD 160 In-stock
50 mg USD 660 In-stock
100 mg USD 1100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MF63

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1[1].

IC50 & Target

mPGES-1[1]

In Vitro

MF63 (0.01-100 µM; 24 h) selectively inhibits PGE2 induced by 10 ng/mL IL-1β in A549 cells, and increases the formation of PGF in a dose-dependent manner[1].
MF63 (10 µM; 24 h) enhances the expression of various metallothionein 1 (MT1) subtypes and endogenous antagonists of IL-1 and IL-36 with the anti-inflammatory effects[2].

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

In Vivo

MF63 (100 mg/kg; p.o.; single dose) attenuates PEG2 accumulation in air pouches and brains of the KI (knock-in mPGES-1 gene) mice and inhibits PEG2 formation in a dose-dependent manner[1].
MF63 (10 mg/kg and 100 mg/kg; p.o.; single dose) inhibits the hyperalgesic response induced by LPS in the KI mice, with dose-dependently manner[1].
MF63 (0-150 mg/kg; p.o.; single dose) inhibits PEG2 synthesis, hyperalgesia, pyresis and relieves Chronic Osteoarthritic-Like Pain in the guinea pig[1].
MF63 (0-100 mg/kg; p.o.; twice daily for 4 days) has gastrointestinal tolerability in KI mice and nonhuman primates[1].

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

Animal Model: 10 to 12 weeks of KI and wild-type mice which injected LPS[1].
Dosage: 10 mg/kg and 100 mg/kg.
Administration: Oral gavage; single dose.
Result: Inhibited the PGE2 accumulation in air pouch and brain of KI mice in a dose-dependent manner, and has selectively in the brain.
Reduced the response of hyperalgesia by 50% at 10 mg/kg and 80% at 100 mg/kg in KI mice but without effecting wild-type mice.
Animal Model: Young male Hartley guinea pigs (~250 g) with osteoarthritic pain[1].
Dosage: 0, 3, 10, 15, 30, 50, 100 or 150 mg/kg.
Administration: Oral gavage; single dose.
Result: Inhibited the formation of PGE2 in a dose-dependent manner, relieved Chronic Osteoarthritic-Like Pain and also inhibited pyresis.
Animal Model: 10 to 12 weeks of KI mice and nonhuman primates[1].
Dosage: 0, 3, 10, 30 or 100 mg/kg.
Administration: Oral gavage; twice daily for 4 days.
Result: Had no gastrointestinal toxicity in KI mice and non-human primates.
Molecular Weight

378.81

Formula

C23H11ClN4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC(C2=C3C=CC=C2)=C(C4=C3N=C(C5=C(C=CC=C5C#N)C#N)N4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (197.99 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 2.6398 mL 13.1992 mL 26.3985 mL
5 mM 0.5280 mL 2.6398 mL 5.2797 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, 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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 (6.60 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 (6.60 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:

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.
 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: 99.55%

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, 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
DMSO 1 mM 2.6398 mL 13.1992 mL 26.3985 mL 65.9961 mL
5 mM 0.5280 mL 2.6398 mL 5.2797 mL 13.1992 mL
10 mM 0.2640 mL 1.3199 mL 2.6398 mL 6.5996 mL
15 mM 0.1760 mL 0.8799 mL 1.7599 mL 4.3997 mL
20 mM 0.1320 mL 0.6600 mL 1.3199 mL 3.2998 mL
25 mM 0.1056 mL 0.5280 mL 1.0559 mL 2.6398 mL
30 mM 0.0880 mL 0.4400 mL 0.8799 mL 2.1999 mL
40 mM 0.0660 mL 0.3300 mL 0.6600 mL 1.6499 mL
50 mM 0.0528 mL 0.2640 mL 0.5280 mL 1.3199 mL
60 mM 0.0440 mL 0.2200 mL 0.4400 mL 1.0999 mL
80 mM 0.0330 mL 0.1650 mL 0.3300 mL 0.8250 mL
100 mM 0.0264 mL 0.1320 mL 0.2640 mL 0.6600 mL
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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.

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MF63
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