Home GPCR & G Protein OX Receptor antagonist SB408124

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SB408124 OX Receptor antagonist

Cat.No.S1545

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.
SB408124 OX Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 356.37

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Batch: S154501 DMSO]36 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.74%
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99.74

Solubility

In vitro
Batch:

DMSO : 36 mg/mL (101.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 356.37 Formula

C19H18F2N4O

 Storage (From the date of receipt)
CAS No. 288150-92-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC(=C2C=C(C=C(C2=N1)F)F)NC(=O)NC3=CC=C(C=C3)N(C)C

Mechanism of Action

Targets/IC50/Ki
OX1 (membrane)
27 nM(Ki)
OX1 (whole cell)
57 nM(Ki)
In vitro
SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production.
In vivo
SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP).
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/19592616/

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