VU0530244

VU0530244 is a potent antagonist of 5-HT2B, with the IC50 of 17.3 nM. VU0530244 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans[1].

Product Specifications

CAS Number

[1396886-30-8]

UNSPSC

12352005

Target

5-HT Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Smiles

O=C(N1CC(C1)C2=NC3=C(N2)C=C(C)C=C3)C4=CC(C5=CC=C(F)C=C5)=NN4C

Molecular Formula

C22H20FN5O

Molecular Weight

389.43

References & Citations

[1]Aaron M Bender, et al. Identification of Potent, Selective, and Peripherally Restricted Serotonin Receptor 2B Antagonists from a High-Throughput Screen. Assay Drug Dev Technol. 2023 Apr;21 (3) :89-96.