Art. -Nr.: HY-103088

Palupiprant

(Synonyms: E7046)

3 Cited Publications

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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 K_i of 23.14 nM. Palupiprant exhibits anti-tumor activities.

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Reinheit: 99.96%
CAS. Nr.: 1369489-71-3
Formel: C₂₂H₁₈F₅N₃O₄
Molecular Weight:483.39

Speicherung:

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

Palupiprant Chemical Structure

CAS. Nr.: 1369489-71-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC₅₀ of 13.5 nM and K_i of 23.14 nM. Palupiprant exhibits anti-tumor activities^[1]^[2].

IC₅₀ & Target

IC50: 13.5 nM (EP4)^[2]
Ki: 23.14 nM (EP4)^[2]

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
3LL cell line	IC₅₀	>100 μM Compound: 4; E7046	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	[PMID: 35640059]
4T1	IC₅₀	>100 μM Compound: 6; E7046	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	[PMID: 37312837]
CHO	IC₅₀	>10000 nM Compound: 4; E7046	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	[PMID: 31855426]
CHO	IC₅₀	>10000 nM Compound: 4; E7046	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	[PMID: 31855426]
CHO	IC₅₀	181.1 nM Compound: 4; E7046	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	[PMID: 31855426]
CHO	IC₅₀	7.5 nM Compound: 4; E7046	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	[PMID: 31855426]
CHO	IC₅₀	>10000 nM Compound: 4; E7046	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	[PMID: 31855426]
CT26	IC₅₀	>100 μM Compound: 4; E7046	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	[PMID: 35640059]
CT26.WT	IC₅₀	>100 μM Compound: 6; E7046	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	[PMID: 37312837]
EMT6	IC₅₀	>100 μM Compound: 4; E7046	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	[PMID: 35640059]
HEK293	IC₅₀	>100 μM Compound: 4; E7046	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	[PMID: 35640059]
Lewis lung carcinoma cell line	IC₅₀	>100 μM Compound: 6; E7046	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	[PMID: 37312837]
MCF7	IC₅₀	>100 μM Compound: 6; E7046	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	[PMID: 37312837]
Panc02	IC₅₀	>100 μM Compound: 4; E7046	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	[PMID: 35640059]

In Vitro

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.

In Vivo

In the CT-26 tumor model, the Palupiprant/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of Palupiprant and RT also produces significant better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors^[1]. Palupiprant (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. Blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. Palupiprant treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells. Furthermore, co-administration of Palupiprant and E7777, an IL-2-diphtheria toxin fusion protein that preferentially kills Tregs, synergistically disrupts the myeloid and Treg immunosuppressive networks, resulting in effective and durable anti-tumor immune responses in mouse tumor models^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1369489-71-3
Appearance Solid
Molecular Weight 483.39
Formel C₂₂H₁₈F₅N₃O₄
Color White to off-white
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
Synonyms

E7046
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Lösungsmittel & Löslichkeit

In Vitro:

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.

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

2.0687 mL

10.3436 mL

20.6872 mL

5 mM

0.4137 mL

2.0687 mL

4.1374 mL

10 mM

0.2069 mL

1.0344 mL

2.0687 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.08 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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 + +
%
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

Protokoll

Cell Assay^[2]

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.

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
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)
Handling Instructions (2659 KB)

Verweise

[1]. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics

[2]. Diana I. Albu, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. Oncoimmunology. 2017 Jun 28;6(8):e1338239. [Content Brief]

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	2.0687 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

Keywords

Palupiprant

3 Cited Publications

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Palupiprant

GPCR/G Protein Compound Library

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Anti-Cancer Compound Library

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Angiogenesis-Related Compound Library

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Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Palupiprant

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Palupiprant

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Palupiprant

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Palupiprant Related Classifications

HY-103088 Related Classifications