Vorbipiprant

Vorbipiprant (CR6086) is an orally active EP4 receptor antagonist with high selectivity for the human EP4 receptor (Ki: 16.6 nM) . Vorbipiprant has immunomodulatory, anti-inflammatory, antitumor, and anti-angiogenic activities. Vorbipiprant can inhibit the expression of multiple pro-inflammatory cytokines and the activation of immune cells, and convert "cold" tumors unresponsive to immune checkpoint inhibitors into "hot" tumors. Vorbipiprant is used in the research of diseases such as rheumatoid arthritis and colon cancer[1][2].

Product Specifications

CAS Number

[1417742-86-9]

Product Name Alternative

CR6086

UNSPSC

12352005

Target

Interleukin Related; MMP; PD-1/PD-L1; Prostaglandin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/vorbipiprant.html

Purity

99.72

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C2(CC2)NC(C3N(CCC4(C3)CC4)CC5=CC=C(C(F)(F)F)C=C5)=O)C=C1)O

Molecular Formula

C26H27F3N2O3

Molecular Weight

472.50

References & Citations

[1]Caselli G, et al. Pharmacological characterisation of CR6086, a potent prostaglandin E2 receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug. Arthritis Res Ther. 2018 Mar 1;20 (1) :39.|[2]Caselli G, et al. Combination of the EP4 antagonist CR6086 and anti-PD-1 monoclonal antibody inhibits tumor growth in a microsatellite stable colorectal cancer in mice. Cancer Research, 2020, 80 (16_Supplement) : 2208-2208.