Palupiprant
Based on 3 publication(s) in Google Scholar
Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. Palupiprant exhibits anti-tumor activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.96%
- No. CAS: 1369489-71-3
- Fòrmula: C22H18F5N3O4
- Peso molecular:483.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Palupiprant
More
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 3LL cell line | IC50 |
>100 μM
Compound: 4; E7046
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Cytotoxicity against mouse 3LL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse 3LL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 35640059] |
| 4T1 | IC50 |
>100 μM
Compound: 6; E7046
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Cytotoxicity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
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[PMID: 37312837] |
| CHO | IC50 |
>10000 nM
Compound: 4; E7046
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Antagonist activity at human EP2 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
Antagonist activity at human EP2 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
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[PMID: 31855426] |
| CHO | IC50 |
>10000 nM
Compound: 4; E7046
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Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
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[PMID: 31855426] |
| CHO | IC50 |
181.1 nM
Compound: 4; E7046
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Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
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[PMID: 31855426] |
| CHO | IC50 |
7.5 nM
Compound: 4; E7046
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Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
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[PMID: 31855426] |
| CHO | IC50 |
>10000 nM
Compound: 4; E7046
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Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay
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[PMID: 31855426] |
| CT26 | IC50 |
>100 μM
Compound: 4; E7046
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Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 35640059] |
| CT26.WT | IC50 |
>100 μM
Compound: 6; E7046
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Cytotoxicity against mouse CT26.WT cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse CT26.WT cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
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[PMID: 37312837] |
| EMT6 | IC50 |
>100 μM
Compound: 4; E7046
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Cytotoxicity against mouse EMT6 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse EMT6 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 35640059] |
| HEK293 | IC50 |
>100 μM
Compound: 4; E7046
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Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 35640059] |
| Lewis lung carcinoma cell line | IC50 |
>100 μM
Compound: 6; E7046
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Cytotoxicity against mouse Lewis lung carcinoma cell line assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse Lewis lung carcinoma cell line assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
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[PMID: 37312837] |
| MCF7 | IC50 |
>100 μM
Compound: 6; E7046
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Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
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[PMID: 37312837] |
| Panc02 | IC50 |
>100 μM
Compound: 4; E7046
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Cytotoxicity against mouse Panc02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse Panc02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 35640059] |
Palupiprant (E7046) reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1369489-71-3
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Appearance Solid
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Peso molecular 483.39
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Fòrmula C22H18F5N3O4
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Color White to off-white
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SMILES
O=C(O)C1=CC=C([C@@H](NC(C2=C(OC3=CC=CC(C(F)(F)F)=C3)N(C)N=C2C(F)F)=O)C)C=C1
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Synonyms
E7046
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Biomed Sci
Exosomal PGE2 from M2 macrophages inhibits neutrophil recruitment and NET formation through lipid mediator class switching in sepsis. [Abstract]2023 Aug 2;30(1):62. PMID: 37533081 -
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 -
Cancer Res Commun
Dual Blockade of EP2 and EP4 Signaling is Required for Optimal Immune Activation and Antitumor Activity Against Prostaglandin-Expressing Tumors. [Abstract]2023 Aug 8;3(8):1486-1500. PMID: 37559947
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (206.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.08 mg/mL (4.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocolo
Bone marrow (BM) cells are flushed from femurs of BALB/c mice using sterile CM. Freshly harvested (BM) cells (0.5×106) are differentiated in the presence of 20 ng/mL recombinant mouse GM-CSF, ±PGE2 (10 nM), at 37°C, for 8 d. CM C fresh GM-CSF ± PGE2 is changed on days 3 and 6. After in vitro differentiation, cells are analyzed by flow cytometry. For certain experiments, CT26, 4T1 cell supernatants, and/or EP1 (SC-57089), EP2 (ER-880696), EP3 (L-798106), or EP4 (E7046) antagonists at 1 mM, are added to the BM cells. To assess the effect of differentiated BM cells on T cell proliferation, mouse BM cells differentiated are co-cultured for 72 hours with anti-CD3/CD28 Dynabeadsstimulated and CFSE (1 mM)-stained T cells. T cell proliferation is assessed by CFSE dilution using flow cytometry.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For the tumor isograft efficacy studies, 6-week old female BALB/c mice are implanted with cancer cells: 1×105 CT26 or 4T1 cells or 8×105 H22 cells per mouse s.c., or 1×105 EMT6 cells in the mammary fat pad. C57BL/6 mice are implanted s.c. with 1×106 Pan02 cells per mouse, and A/J mice are implanted s.c. with 2-3 mm3 SAI/N tumor fragments. To investigate the role of T cells in the anti-tumor response, 6 week old female nude mice (which lack T cells) are injected s.c. with 1×105 CT26 cells. When tumors reach approximately 50-100 mm3, tumor-bearing mice are randomly assigned to vehicle or treatment groups, and treatment regimens begin. E7046 is administered per oral (p.o.) as a 100 or 150 mg/kg suspension in 0.5% MC, daily for 21 d (QDx21). For the combination studies, E7777 is administered intravenously (i.v.) at 2.5 mg/mouse in saline, as 2 to 3 doses injected one week apart (Q7Dx2-3). Tumor volumes and body weights are recorded 2-3 times a week. For comparison with current immunotherapies, in addition to vehicle control and E7046 C E7777 groups, mice are assigned to anti-PD1 antibodies or anti-mouse PD-1 C antimouse CTLA4 antibodies treatment groups. Anti-PD-1 and anti-CTLA-4 antibodies (1 mg/mL), are administered i.p. in 100 mL, 3 times 4 d apart (Q4Dx3) for a total of 300 mg each. Isotype controls are administered i.p. at 1 mg/mL to the control group. For the CD4CT and CD8CT lymphocyte depletion, antimouse CD4 or anti-mouse CD8 antibodies or their isotype controls are administered in 100 mL, i.p. at 2.5 mg/mL every 4 days, for a total of 4 injections per mouse (1 mg).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.0687 mL | 10.3436 mL | 20.6872 mL | 51.7181 mL |
| 5 mM | 0.4137 mL | 2.0687 mL | 4.1374 mL | 10.3436 mL | |
| 10 mM | 0.2069 mL | 1.0344 mL | 2.0687 mL | 5.1718 mL | |
| 15 mM | 0.1379 mL | 0.6896 mL | 1.3791 mL | 3.4479 mL | |
| 20 mM | 0.1034 mL | 0.5172 mL | 1.0344 mL | 2.5859 mL | |
| 25 mM | 0.0827 mL | 0.4137 mL | 0.8275 mL | 2.0687 mL | |
| 30 mM | 0.0690 mL | 0.3448 mL | 0.6896 mL | 1.7239 mL | |
| 40 mM | 0.0517 mL | 0.2586 mL | 0.5172 mL | 1.2930 mL | |
| 50 mM | 0.0414 mL | 0.2069 mL | 0.4137 mL | 1.0344 mL | |
| 60 mM | 0.0345 mL | 0.1724 mL | 0.3448 mL | 0.8620 mL | |
| 80 mM | 0.0259 mL | 0.1293 mL | 0.2586 mL | 0.6465 mL | |
| 100 mM | 0.0207 mL | 0.1034 mL | 0.2069 mL | 0.5172 mL |
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