SB-674042

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively[1][4].

Product Specifications

CAS Number

[483313-22-0]

UNSPSC

12352005

Hazard Statement

H302

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/SB-674042.html

Purity

99.93

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

FC1=C(C2=C(C(N3[C@H](CC4=NN=C(C5=CC=CC=C5)O4)CCC3)=O)N=C(C)S2)C=CC=C1

Molecular Formula

C24H21FN4O2S

Molecular Weight

448.51

Precautions

H302

References & Citations

[1]Langmead CJ, et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141 (2) :340-6. |[2]Ellis J, et al. Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. J Biol Chem. 2006 Dec 15;281 (50) :38812-24. |[3]Chang X, et al. Orexin-A Stimulates Insulin Secretion Through the Activation of the OX1 Receptor and Mammalian Target of Rapamycin in Rat Insulinoma Cells. Pancreas. 2019 Apr;48 (4) :568-573. |[4]Yaeger JDW, et al. Orexin 1 Receptor Antagonism in the Basolateral Amygdala Shifts the Balance From Pro- to Antistress Signaling and Behavior. Biol Psychiatry. 2022 May 1;91 (9) :841-852.