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Art. -Nr.: HY-10952

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ONO-AE2-227

ONO-AE2-227 is an orally active EP4 receptor antagonist. ONO-AE2-227 blocks PGE2-mediated EP4 signaling by competitively antagonizing PGE2-induced cAMP elevation, and binds to EP4/EP3 with mouse K_i values of 2.7/21 nM. ONO-AE2-227 reduces aberrant crypt foci and intestinal polyp development, and inhibits intestinal polyp formation. ONO-AE2-227 enhances LPS-induced TNF-alpha release from human alveolar macrophages by blocking endogenous PGE2, blocks PGE2-induced ICAM-1 expression and leukocyte-endothelial adhesion, and attenuates PGE2-induced monocyte adhesion to brain endothelial cells. ONO-AE2-227 can be used for research on colon cancer.

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CAS. Nr.: 357605-73-3
Formel: C₂₇H₂₃NO₃
Molecular Weight:409.49

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ONO-AE2-227 Chemical Structure

CAS. Nr.: 357605-73-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[2]^[3]

EP4

2.7 nM (Ki)

EP2

21 nM (Ki)

TNF-α

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In Vitro

Innate ImmunityCytokines & ChemokinesLipid Inflammatory MediatorsLocal Vascular RegulationOthers

Innate Immunity

Cytokines & Chemokines

Lipid Inflammatory Mediators

ONO-AE2-227 (10-1000 nM; 20 min before PGE2 and 24 h with LPS) in human MDMs acts as an EP4 antagonist that right-shifts PGE2 inhibition of LPS-induced TNF-α release with a non-simple-competitive slope of 0.53^[3].

Lipid Inflammatory Mediators

Local Vascular Regulation

ONO-AE2-227 blocks PGE2-induced ICAM-1 expression in bEnd.3 brain endothelial cells^[4].
ONO-AE2-227 (10 mM; 24 h) reduces PGE2-induced ICAM-1 protein expression in primary cultured mouse brain endothelial cells^[4].
ONO-AE2-227 (10 mM; 24 h) eliminates PGE2-induced U937 monocyte adhesion to bEnd.3 brain endothelial cells^[4].

Others

ONO-AE2-227 antagonizes PGE2-induced cAMP accumulation in mouse recombinant EP4/CHO cells with a pIC₅₀ of 8.0^[1].
ONO-AE2-227 (2.7-21 nM) binds mouse EP4 with a K_i of 2.7 nM and mouse EP3 with a K_i of 21 nM in CHO cell binding assays, with 1000-fold lower affinity for mouse EP1, EP2, DP, FP, IP, and TP^[2].
ONO-AE2-227 (10-160 nM) is a potent competitive EP4 antagonist (10 nM median inhibitory concentration for PGE2-induced cAMP increase) and a weak EP3 antagonist (160 nM IC₅₀ for PGE2-induced calcium increase) in receptor-expressing cell assays^[2].
ONO-AE2-227 (15 min) is a potent EP4 receptor antagonist (pK_B 9.17) with high selectivity over EP2 in transfected HEK cells^[3].

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

In Vivo

Anti-cancer

ONO-AE2-227 (100-400 ppm; p.o.; ad libitum; from the day before the first AOM administration to week 5) reduced Azoxymethane (AOM) (HY-111375)-induced colonic ACF formation in C57BL/6Cr mice at higher doses, whereas lower doses had no such effect^[2].
ONO-AE2-227 (300 ppm; p.o.; ad libitum; from 6 weeks of age for 7 weeks) reduced the total number of intestinal polyps in Min mice, with the most significant reduction in the distal small intestine^[2].

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

Animal Model:

C57BL/6Cr (male, 6 weeks of age)^[2]
Dosage:

100 or 400 ppm in diet
Administration:

p.o.; ad libitum; from the day before first AOM until week 5
Result:

In AOM-treated mice (n = 8 per group), 400 ppm ONO-AE2-227 reduced ACFs/colon to 8.3 (67% of the AOM-alone group), and the mean number of ACs/focus was 1.5.
The 100 ppm ONO-AE2-227 group had 12.4 ACFs/colon and 1.5 mean ACs/focus and did not affect ACF formation.
No ACFs were observed in vehicle-injected mice with or without 400 ppm ONO-AE2-227.

Animal Model:

C57BL/6J-Min/+ (female, 6 weeks of age)^[2]
Dosage:

300 ppm in diet
Administration:

p.o.; ad libitum; from 6 weeks of age for 7 weeks
Result:

In Min mice treated with 300 ppm ONO-AE2-227, total polyps/mouse were 42.2 (69% of the basal diet group).
By location, polyp numbers/mouse were: proximal small intestine 3.3 (83%), middle small intestine 14.2 (74%), distal small intestine 24.5 (65%), and colon 0.2 (40%).
The size distribution showed reduction in polyps measuring ≤1.0 mm in diameter but not those >1.0 mm in diameter.

Related Protocols :

Chemical Information

CAS. Nr. 357605-73-3
Molecular Weight 409.49
Formel C₂₇H₂₃NO₃
SMILES

O=C(O)C=1C=CC=CC1CC=2C=CC=CC2NC(=O)C(C3=CC=CC=4C=CC=CC43)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Jones RL, et al. Prostanoid receptor antagonists: development strategies and therapeutic applications. British journal of pharmacology. 2009 Sep;158(1):104-45.

[2]. Mutoh M, et al. Involvement of prostaglandin E receptor subtype EP(4) in colon carcinogenesis. Cancer Res. 2002 Jan 1;62(1):28-32.

[3]. Ratcliffe MJ, et al. Activation of E-prostanoid4 and E-prostanoid2 receptors inhibits TNF-alpha release from human alveolar macrophages. The European respiratory journal. 2007 May;29(5):986-94.

[4]. Park TY, et al. Prostaglandin E₂-induced intercellular adhesion molecule-1 expression is mediated by cAMP/Epac signalling modules in bEnd.3 brain endothelial cells. British journal of pharmacology. 2013 Jun;169(3):604-18.

Calculators

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)}

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.

Bioz

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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ONO-AE2-227

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