APJ antagonist-1

APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC50 of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis[1].

Product Specifications

UNSPSC

12352005

Target

Apelin Receptor (APJ)

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=S(C1=CC=C([N+]([O-])=O)C=C1)(OC2=CC(CSC3=NC=CC=N3)=CC=C2OC)=O

Molecular Formula

C18H15N3O6S2

Molecular Weight

433.46

References & Citations

[1]Bist G, et al. Novel small molecule analogs for advancing apelin receptor antagonism with enhanced plasma and microsomal stability. Bioorg Med Chem Lett. 2025 Aug 8;129:130367.