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SB-674042

Catalog No. T16854 CAS 483313-22-0

Synonyms: SB674042

SB-674042 is a potent and selective dual antagonist of the non-peptide orexigenic peptides OX1 and OX2 receptors, with IC50s of 3.76 nM and 531 nM, respectively.SB-674042 can be used for the treatment of depression.

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SB-674042, CAS 483313-22-0

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2 mg	In stock	$ 84.00

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Purity: 99.9%

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Chemical Properties

Storage & Solubility Information

Description	SB-674042 is a potent and selective dual antagonist of the non-peptide orexigenic peptides OX1 and OX2 receptors, with IC50s of 3.76 nM and 531 nM, respectively.SB-674042 can be used for the treatment of depression.
In vitro	[(3)H]SB-674042 is a specific, high-affinity radioligand for the OX(1) receptor. Specific binding of [(3)H]SB-674042 was saturable in both whole cell and membrane formats. Analyses suggested a single high-affinity site, with K(d) values of 3.76+/-0.45 and 5.03+/-0.31 nM[1]。Treatment of cells co-expressing the orexin-1 and CB1 receptors with the orexin-1 receptor antagonist SB-674042 also resulted in re-localization of both receptors to the cell surface. Treatment with SB-674042 also reduced the potency of a CB1 receptor agonist to phosphorylate ERK1/2 only when the two receptors were co-expressed[4].
In vivo	In the Stress Alternatives Model (SMA) in mice, administration of SB-674042 at a dose of 0.3 nM/0.3 μL via icv (intracerebroventricular injection) reduces contextual and cue fear freezing responses in Stay animals[2].

Synonyms	SB674042
Molecular Weight	448.51
Formula	C24H21FN4O2S
CAS No.	483313-22-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 20 mg/mL (44.59 mM), Sonication is recommended.

References and Literature

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. 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. 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. 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.

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Keywords

SB-674042 483313-22-0 GPCR/G Protein Neuroscience OX Receptor SB674042 SB 674042 inhibitor inhibit

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