L-732138

L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action[1][2].

Product Specifications

CAS Number

[148451-96-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/l-732138.html

Concentration

10mM

Purity

99.9

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(OCC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)[C@H](CC2=CNC3=CC=CC=C23)NC(C)=O

Molecular Formula

C22H18F6N2O3

Molecular Weight

472.38

Precautions

H302, H315, H319, H335

References & Citations

[1]Muñoz M, et al. The NK-1 Receptor Antagonist L-732,138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. Cancers (Basel) . 2010 Apr 20;2 (2) :611-23.|[2]Cascieri MA, et al. Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. J Biol Chem. 1994 Mar 4;269 (9) :6587-91.|[3]Kuo HP, et al. Lipopolysaccharide enhances neurogenic plasma exudation in guinea-pig airways. Br J Pharmacol. 1998 Oct;125 (4) :711-6.