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SB-674042

CAT: 0804-HY-10898-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10898-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
OX1 Receptor; OX2 Receptor