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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
5-HT2 Receptor; α-1 microglobulin
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