SB 235375

SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models[1].

Product Specifications

CAS Number

[224961-34-6]

UNSPSC

12352005

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/sb-235375.html

Purity

98.13

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N[C@H](C1=CC=CC=C1)CC)C2=C(C(C3=CC=CC=C3)=NC4=CC=CC=C24)OCC(O)=O

Molecular Formula

C27H24N2O4

Molecular Weight

440.49

References & Citations

[1]Giardina GA, et al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S) -N- (1-phenylpropyl) -3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412) . J Med Chem. 1999 Mar 25;42 (6) :1053-65.