Palupiprant (Synonyms: E7046)

Name: Palupiprant
Brand: MedChemExpress
SKU: HY-103088
Rating: 5.0 (3 reviews)

製品番号: HY-103088 純度: 99.96%: Data Sheet SDS COA 取扱説明書
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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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Palupiprant 構造式

CAS 番号 : 1369489-71-3

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 64	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 64	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$60	在庫あり	Estimated Time of Arrival: December 31
10 mg	$84	在庫あり	Estimated Time of Arrival: December 31
25 mg	$156	在庫あり	Estimated Time of Arrival: December 31
50 mg	$276	在庫あり	Estimated Time of Arrival: December 31
100 mg		お問い合わせ
200 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Palupiprant:

Palupiprant (Standard) お問い合わせ

顧客検証

Prostaglandin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

DP EP FP IP TXA₂/TP TXB₂

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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]

Cellular Effect

Cell Line	Type	Value	Description	References
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	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]
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]
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]
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]

体外実験

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.

体内実験

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.

臨床実験

分子量

483.39

分子式

C₂₂H₁₈F₅N₃O₄

CAS 番号

1369489-71-3

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.96%

Select Batch:

データシート (284 KB) SDS (393 KB)

COA (255 KB) HNMR (138 KB) RP-HPLC (225 KB) MS (69 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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]

Complete Stock Solution Preparation Table

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

Palupiprant Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Palupiprant1369489-71-3E7046E 7046E-7046Prostaglandin ReceptorInhibitorinhibitorinhibit

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Palupiprant (Synonyms: E7046)

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Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Palupiprant Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Palupiprant (Synonyms: E7046)

カスタマーレビュー

Other Forms of Palupiprant:

Palupiprant 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Prostaglandin Receptor アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Palupiprant 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Palupiprant Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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