Cat. No.: HY-13283

MF63

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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.

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Pureté: 99.55%
CAS No.: 892549-43-8
Formule: C₂₃H₁₁ClN₄
Masse moléculaire:378.81

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MF63 Chemical Structure

CAS No.: 892549-43-8

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>40 μM Compound: 1	Inhibition of PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum Inhibition of PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum	[PMID: 19748780]
A549	IC₅₀	>50 μM Compound: 1	Inhibition of PGF synthase in IL1-beta treated human A549 cell microsome assessed as inhibition of PGF2alpha production after 1 min in presence of 50% FBS Inhibition of PGF synthase in IL1-beta treated human A549 cell microsome assessed as inhibition of PGF2alpha production after 1 min in presence of 50% FBS	[PMID: 21295979]
A549	IC₅₀	>50 μM Compound: 22	Inhibition of PGE2alpha synthesis in human A549 cells Inhibition of PGE2alpha synthesis in human A549 cells	[PMID: 18459759]
A549	IC₅₀	>50 μM Compound: 3, MF63	Inhibition of IL-1-beta-stimulated PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum Inhibition of IL-1-beta-stimulated PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum	[PMID: 18029174]
A549	IC₅₀	0.42 μM Compound: 1	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsome assessed as inhibition of PGE2 production after 1 min in presence of 50% FBS Inhibition of mPGES1 in IL1-beta treated human A549 cell microsome assessed as inhibition of PGE2 production after 1 min in presence of 50% FBS	[PMID: 21295979]
A549	IC₅₀	0.42 μM Compound: 1	Inhibition of mPGES1 in IL-1-beta-stimulated human A549 cells assessed as blockade of PGH2 to PGE2 conversion in presence of 50% fetal bovine serum Inhibition of mPGES1 in IL-1-beta-stimulated human A549 cells assessed as blockade of PGH2 to PGE2 conversion in presence of 50% fetal bovine serum	[PMID: 19748780]
A549	IC₅₀	0.42 μM Compound: 22	Inhibition of PGE2 synthesis in human A549 cells Inhibition of PGE2 synthesis in human A549 cells	[PMID: 18459759]
A549	IC₅₀	0.42 μM Compound: 3, MF63	Inhibition of IL-1-beta-stimulated PGE2 production in human A549 cells in presence of 50% fetal bovine serum Inhibition of IL-1-beta-stimulated PGE2 production in human A549 cells in presence of 50% fetal bovine serum	[PMID: 18029174]
A549	IC₅₀	56 nM Compound: 1; MF-63	Inhibition of mPGES-1 in human A549 cells assessed as reduction in interleukin-1 beta-induced PGE2 production incubated for 30 mins followed by IL-1beta stimulation for 16 to 20 hrs in presence of 2% fetal bovine serum by HTRF assay Inhibition of mPGES-1 in human A549 cells assessed as reduction in interleukin-1 beta-induced PGE2 production incubated for 30 mins followed by IL-1beta stimulation for 16 to 20 hrs in presence of 2% fetal bovine serum by HTRF assay	[PMID: 27865703]
A549	IC₅₀	56 nM Compound: 1; MF-63	Inhibition of mPGES-1 in human A549 cells assessed as decrease in IL1beta induced PGE2 release preincubated for 30 mins followed by IL-1beta addition after 16 to 20 hrs by HTRF method Inhibition of mPGES-1 in human A549 cells assessed as decrease in IL1beta induced PGE2 release preincubated for 30 mins followed by IL-1beta addition after 16 to 20 hrs by HTRF method	[PMID: 28400234]
A549	IC₅₀	76 nM Compound: 1; MF-63	Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method	[PMID: 26653180]
CHO	IC₅₀	1 nM Compound: 22	Inhibition of human recombinant mPGES1 expressed in CHO cells Inhibition of human recombinant mPGES1 expressed in CHO cells	[PMID: 18459759]
CHO	IC₅₀	1.9 nM Compound: 1; MF-63	Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH	[PMID: 27865703]
CHO-K1	IC₅₀	0.001 μM Compound: 1	Displacement of [3H]PGH2 from human recombinant PGES1 expressed in CHOK1 cells Displacement of [3H]PGH2 from human recombinant PGES1 expressed in CHOK1 cells	[PMID: 19748780]
HEK293	IC₅₀	4.3 nM Compound: MF-63	Inhibition of microsomal PGES1 transfected in human HEK293 cells assessed as PGE2 production after 60 mins by HTRF assay Inhibition of microsomal PGES1 transfected in human HEK293 cells assessed as PGE2 production after 60 mins by HTRF assay	[PMID: 22137787]
Sf9	IC₅₀	1.59 μM Compound: MF63	Inhibition of purified mPGES-1 (1 to 152) (unknown origin) extracted from detergent-solubilized baculovirus-infected insect Sf9 cell membranes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis Inhibition of purified mPGES-1 (1 to 152) (unknown origin) extracted from detergent-solubilized baculovirus-infected insect Sf9 cell membranes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis	[PMID: 25961169]

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_2α 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.

Chemical Information

CAS No. 892549-43-8
Appearance Solid
Masse moléculaire 378.81
Formule C₂₃H₁₁ClN₄
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Research Square Preprint

2023 May 19.

Solvant et solubilité

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)

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

2.6398 mL

13.1992 mL

26.3985 mL

5 mM

0.5280 mL

2.6398 mL

5.2797 mL

10 mM

0.2640 mL

1.3199 mL

2.6398 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, 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.

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)

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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 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.

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:

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mg/kg
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g
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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:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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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 (280 KB)
SDS (251 KB)
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- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Xu D, et al. MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation. J Pharmacol Exp Ther. 2008 Sep;326(3):754-63. [Content Brief]

[2]. Tuure L, et al. Regulation of gene expression by MF63, a selective inhibitor of microsomal PGE synthase 1 (mPGES1) in human osteoarthritic chondrocytes. Br J Pharmacol. 2020 Sep;177(18):4134-4146.

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, 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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MF63

Pyroptosis Compound Library

Orally Active Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Publications Citing Use of MedChemExpress (MCE) MF63

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MF63

Pyroptosis Compound Library

Orally Active Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Publications Citing Use of MedChemExpress (MCE) MF63

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MF63 Related Classifications

HY-13283 Related Classifications