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CAY10789

CAY10789 is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM) . CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases[1].

Product Specifications

CAS Number

[123226-28-8]

UNSPSC

12352005

Target

G protein-coupled Bile Acid Receptor 1; Leukotriene Receptor; TNF Receptor

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/cay10789.html

Purity

99.84

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OCC1=CC=CC(OCC2=NC3=CC=CC=C3C=C2)=C1

Molecular Formula

C17H15NO2

Molecular Weight

265.31

References & Citations

[1]Fiorillo B, et al. Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1. J Med Chem. 2021 Nov 25;64 (22) :16512-16529.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

LTD4/CysLT1; TNFRSF5/CD40

Available Sizes

Curated Selection

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