| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
EP4 receptor (E prostanoid receptor 4).
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|---|---|
| ln Vitro |
In the presence or absence of 10% serum, MF498 (0.01 nM–10 μM, 30 minutes) suppresses PGE2-stimulated cAMP buildup with IC50 values of 1.7 and 17 nM, respectively [1]. In VSMC, MF498 0.01 and 0.1 μM, 30 minutes) suppresses the proliferation of VSMC produced by FBS and PDGF-BB [2]. In VSMC, MF498 (0.1 μM, 30 minutes) suppresses the expression of PCNA and cyclin D1 produced by PDGF [2]. The PDGF-BB-induced migration is inhibited by MF498 (0.1 μM, 30 min) [2].
MF498 inhibits PGE2-stimulated cAMP accumulation in a dose-dependent manner with IC50 values of 1.7 nM and 17 nM in the absence and presence of 10% serum, respectively. It inhibits FBS and PDGF-BB-induced vascular smooth muscle cell (VSMC) proliferation, reduces PDGF-induced cyclin D1 and PCNA expression, and inhibits PDGF-BB-induced migration in rat VSMCs. MF498 displays relatively good selectivity over other prostanoid receptors and does not compromise mucosal integrity in the gastrointestinal tract. |
| ln Vivo |
The Wall Street compound MF498 (0–20 mg/kg) reduces foot swelling in adjuvant-induced arthritis (AIA) [1]. In guinea pigs (L-902688), MF498 (0-30 mg/kg, Wall Street) attenuates EP4 vessels. At a dosage of 1.2 μM, six hours after the laboratory, MF498 (20 mg/kg, buccal) exhibits 100% bioavailability [1].
MF498 relieves joint inflammation and pain in rodent models of rheumatoid arthritis (adjuvant-induced arthritis in rats) and osteoarthritis (iodoacetate-induced joint pain in guinea pigs). Oral administration (0-20 mg/kg) inhibits paw swelling in rats with adjuvant-induced arthritis. It attenuates EP4 agonist-induced hyperalgesia in guinea pigs (0-30 mg/kg, p.o.). |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay measures the displacement of a radiolabeled EP4 ligand from the EP4 receptor in membrane preparations. MF498 is incubated with varying concentrations (typically 0.01 nM to 10 µM) and EP4 receptor-containing membranes. After incubation, bound and free radioactivity are separated by filtration or centrifugation. The Ki value is calculated from competition binding curves using the Cheng-Prusoff equation. For MF498, the Ki for EP4 is 0.7 nM. Selectivity is assessed by profiling against other prostanoid receptors (EP1, EP2, EP3, FP, IP, DP1) and related GPCRs.
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| Cell Assay |
Cell viability assay [2]
Cell Types: Rat VSMC Tested Concentrations: 0.01 nM-10 μM Incubation Duration: 30 minutes before FBS treatment. Experimental Results: Inhibited VSMC proliferation induced by FBS and PDGF-BB. In vitro cellular assays are performed using cells expressing the EP4 receptor, such as human embryonic kidney (HEK) cells or relevant primary cells. Cells are pre-incubated with MF498 (0.01 nM to 10 µM, 30 min) followed by stimulation with PGE2. Intracellular cAMP levels are measured using a competitive immunoassay (e.g., ELISA or HTRF). The IC50 for inhibition of PGE2-stimulated cAMP accumulation is determined. Additionally, the effect of MF498 on cell proliferation (e.g., VSMCs) is assessed by BrdU incorporation or cell counting assays following stimulation with FBS or PDGF-BB. |
| Animal Protocol |
Animal/Disease Models: Adjuvant-Induced Arthritis (AIA) in Rats[1]
Doses: 0, 0.008, 0.04, 0.2, 2, 20 mg/kg Route of Administration: Oral (po) Experimental Results: In primary and secondary paws All demonstrated anti-inflammatory effects. In vivo efficacy is evaluated in the adjuvant-induced arthritis (AIA) rat model and the iodoacetate-induced osteoarthritis guinea pig model. For the AIA model, rats are immunized with complete Freund's adjuvant. MF498 is administered orally at doses ranging from 0 to 20 mg/kg. Paw swelling is measured using a plethysmometer. For the osteoarthritis pain model, guinea pigs receive intra-articular injection of iodoacetate. MF498 (0-30 mg/kg, p.o.) is administered, and hyperalgesia is assessed by measuring paw withdrawal thresholds. |
| ADME/Pharmacokinetics |
MF498 is orally active with 100% bioavailability at 20 mg/kg oral dose, achieving a plasma concentration of 1.2 µM at 6 hours post-dose. The compound is formulated in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline for in vivo administration. The molecular weight is 603.69 g/mol, and the compound is soluble in DMSO (31 mg/mL). MF498 is stable as a powder at -20°C for up to 3 years and in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for MF498. However, the compound is reported to not compromise mucosal integrity in the gastrointestinal tract. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments would typically include acute toxicity studies, hERG channel inhibition assays, and CYP450 enzyme inhibition profiling to assess potential drug-drug interactions and cardiac safety risks.
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| References |
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| Additional Infomation |
MF498 is a research-grade chemical probe for studying EP4 receptor biology in inflammation and pain. It is not approved for clinical use and is available only for preclinical research purposes. The compound is supplied as a powder and should be stored desiccated at -20°C. MF498 is synthesized as a small-molecule antagonist with molecular formula C32H33N3O7S and molecular weight 603.69. It is typically used at concentrations ranging from nanomolar to low micromolar in both in vitro and in vivo studies.
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| Molecular Formula |
C32H33N3O7S
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|---|---|
| Molecular Weight |
603.69
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| Exact Mass |
603.203
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| CAS # |
915191-42-3
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| PubChem CID |
15948325
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| Appearance |
Pink to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.630
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| LogP |
4.64
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
43
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WVLIUERFVJYBNY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H33N3O7S/c1-5-41-30-23-11-9-15-33-29(23)31(42-6-2)24-18-35(32(37)28(24)30)25-14-13-21(16-20(25)3)19-43(38,39)34-27(36)17-22-10-7-8-12-26(22)40-4/h7-16H,5-6,17-19H2,1-4H3,(H,34,36)
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| Chemical Name |
N-[[4-(5,9-diethoxy-6-oxo-8H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methylsulfonyl]-2-(2-methoxyphenyl)acetamide
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| Synonyms |
MF-498; MF 498; MF498
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 31 mg/mL (~51.35 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6565 mL | 8.2824 mL | 16.5648 mL | |
| 5 mM | 0.3313 mL | 1.6565 mL | 3.3130 mL | |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6565 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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