PF-04418948
Based on 12 publication(s) in Google Scholar
PF-04418948, a chemical probe, is an orally active, potent and selective prostaglandin EP2 receptor antagonist with an IC50 of 16 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.40%
- CAS No.: 1078166-57-0
- Formule: C23H20FNO5
- Masse moléculaire:409.41
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) PF-04418948
More- Cancer Discov. 2026 Apr 8. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Antioxidants. 2024 Dec 21;13(12):1579. [Abstract]
- Brain Behav Immun. 2021 Nov:98:337-348. [Abstract]
- J Med Chem. 2025 Jan 23;68(2):1587-1607. [Abstract]
- Neurosci Bull. 2023 Dec;39(12):1775-1788. [Abstract]
- Int J Mol Sci. 2024 Oct 21;25(20):11307. [Abstract]
- Mucosal Immunol. 2025 Apr;18(2):418-430. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Jun;1871(5):167801. [Abstract]
- Genes Immun. 2026 Mar 10. [Abstract]
- J Virol. 2018 Sep 26;92(20):e01018-18. [Abstract]
- Research Square Preprint. 2023 May 19.
Customer Validation & Images
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RT-PCR
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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Histological Imaging/Staining
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RT-PCR
Activité biologique
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EP2 16 nM (IC50) |
PF-04418948 (2 μM; 90 min) inhibits prostaglandin E2 (PGE2)-induced increase in cAMP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO cells
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Concentration:2 μM
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Incubation Time:90 min
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Result:Inhibited prostaglandin E2 (PGE2)-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley rats[1]
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Dosage:1, 3, and 10 mg/kg
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Administration:Oral gavage; 1, 3, and 10 mg/kg; once
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Result:Reduced the peak and AUC butaprost-induced cutaneous blood flow response in a dose-dependent fashion.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1078166-57-0
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Appearance Solid
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Masse moléculaire 409.41
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Formule C23H20FNO5
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Color White to off-white
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SMILES
O=C(C1(COC2=CC=C3C=C(OC)C=CC3=C2)CN(C(C4=CC=C(F)C=C4)=O)C1)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Cancer Discov
Arachidonic Acid Metabolism in PMN-MDSCs Suppresses Antitumor Capacity of T cells in KRAS-Mutant Cholangiocarcinoma. [Abstract]2026 Apr 8. PMID: 41949259 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Antioxidants
2024 Dec 21;13(12):1579. PMID: 39765906 -
Brain Behav Immun
Elevated β-secretase 1 expression mediates CD4+ T cell dysfunction via PGE2 signalling in Alzheimer's disease. [Abstract]2021 Nov:98:337-348. PMID: 34500034 -
J Med Chem
Subtle Structural Modifications Spanning from EP4 Antagonism to EP2/EP4 Dual Antagonism: A Novel Class of Thienocyclic-Based Derivatives. [Abstract]2025 Jan 23;68(2):1587-1607. PMID: 39757828 -
Neurosci Bull
Improving Blood Monocyte Energy Metabolism Enhances Its Ability to Phagocytose Amyloid-β and Prevents Alzheimer's Disease-Type Pathology and Cognitive Deficits. [Abstract]2023 Dec;39(12):1775-1788. PMID: 37316674 -
Int J Mol Sci
Proliferative Diabetic Retinopathy Microenvironment Drives Microglial Polarization and Promotes Angiogenesis and Fibrosis via Cyclooxygenase-2/Prostaglandin E2 Signaling. [Abstract]2024 Oct 21;25(20):11307. PMID: 39457089 -
Mucosal Immunol
Targeting the EP2 receptor ameliorates inflammatory bowel disease in mice by enhancing the immunosuppressive activity of Treg cells. [Abstract]2025 Apr;18(2):418-430. PMID: 39746548
PF-04418948 purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2025 Apr;18(2):418-430. [Abstract]
EP2 antagonist PF-04418948 (0.5 μM) induced an increase in GzmB expression in Treg cells.
PF-04418948 purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2025 Apr;18(2):418-430. [Abstract]
PKA kinase activity assay showing the effect of PF-04418948 (0.5 μM) on the PKA activity in mouse Treg cells.
PF-04418948 purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2025 Apr;18(2):418-430. [Abstract]
PF-04418948 (10 mg/kg; i.p.; once daily for 10 d) administration significantly improved DSS-induced colon shortening in C57BL/6J mice.
PF-04418948 purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2025 Apr;18(2):418-430. [Abstract]
PF-04418948 (10 mg/kg; i.p.; once daily for 10 d) protected DSS-challenged mice from excessive inflammatory responses and intestinal tissue damage.
PF-04418948 purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2025 Apr;18(2):418-430. [Abstract]
PF-04418948 (10 nM-1 μM) significantly increased the expression of GzmB in Treg cells in a dose-dependent manner.
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Biochim Biophys Acta Mol Basis Dis
Prostaglandin E2 alleviates inflammatory response and lung injury through EP4/cAMP/IKK/NF-κB pathway. [Abstract]2025 Jun;1871(5):167801. PMID: 40090625 -
Genes Immun
MTA1-mediated transcriptional repression of Cox2 confers resistance against neutrophil infiltration in endometritis. [Abstract]2026 Mar 10. PMID: 41807815 -
J Virol
Nonsteroidal Anti-inflammatory Drugs Potently Inhibit the Replication of Zika Viruses by Inducing the Degradation of AXL. [Abstract]2018 Sep 26;92(20):e01018-18. PMID: 30068645
PF-04418948 purchased from MedChemExpress. Usage Cited in: J Virol. 2018 Sep 26;92(20):e01018-18. [Abstract]
A549 cells are added with an EP2 or an EP4 inhibitor. After 48 h, cells are subjected to WB with an anti-Axl antibody.
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Solvant et solubilité
DMSO : 50 mg/mL (122.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.11 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.11 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. af Forselles KJ, et al. In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br J Pharmacol. 2011 Dec;164(7):1847-1856. [Content Brief]
[2]. Birrell MA, et al. Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor. Br J Pharmacol. 2013 Jan;168(1):129-138. [Content Brief]
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 |
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| DMSO | 1 mM | 2.4425 mL | 12.2127 mL | 24.4254 mL | 61.0635 mL |
| 5 mM | 0.4885 mL | 2.4425 mL | 4.8851 mL | 12.2127 mL | |
| 10 mM | 0.2443 mL | 1.2213 mL | 2.4425 mL | 6.1063 mL | |
| 15 mM | 0.1628 mL | 0.8142 mL | 1.6284 mL | 4.0709 mL | |
| 20 mM | 0.1221 mL | 0.6106 mL | 1.2213 mL | 3.0532 mL | |
| 25 mM | 0.0977 mL | 0.4885 mL | 0.9770 mL | 2.4425 mL | |
| 30 mM | 0.0814 mL | 0.4071 mL | 0.8142 mL | 2.0354 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6106 mL | 1.5266 mL | |
| 50 mM | 0.0489 mL | 0.2443 mL | 0.4885 mL | 1.2213 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4071 mL | 1.0177 mL | |
| 80 mM | 0.0305 mL | 0.1527 mL | 0.3053 mL | 0.7633 mL | |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2443 mL | 0.6106 mL |
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