SB 218795

SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit[1][2].

Product Specifications

CAS Number

[174635-53-1]

UNSPSC

12352005

Hazard Statement

H302-H315-H319

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-218795.html

Concentration

10mM

Purity

99.86

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

COC([C@@H](C1=CC=CC=C1)NC(C2=CC(C3=CC=CC=C3)=NC4=CC=CC=C24)=O)=O

Molecular Formula

C25H20N2O3

Molecular Weight

396.44

Precautions

P264-P270-P280-P302+P352-P305+P351+P338-P330-P362+P364-P501

References & Citations

[1]Giardina GA, et, al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J Med Chem. 1997 Jun 6;40 (12) :1794-807.|[2]Medhurst AD, et, al. In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br J Pharmacol. 1997 Oct;122 (3) :469-76.|[3]Valero MS, et, al. Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin. 2011 Apr;32 (4) :487-94.