SB-408124

SKU: orb1685631

Description

SB408124 is a potent and selective small molecule antagonist of the orexin-1 (OX1) receptor, exhibiting Ki values of 57 nM and 27 nM in whole cell and membrane assays, respectively, with 50-fold selectivity over the OX2 receptor. This compound is a valuable research tool for investigating orexin system function in sleep, addiction, and stress-related behaviors in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 288150-92-5
• MW: 356.37
• Purity: 99.81%
• Formula: C₁₉H₁₈F₂N₄O
• SMILES: CN(C)c1ccc(NC(=O)Nc2cc(C)nc3c(F)cc(F)cc23)cc1
• Target: OX Receptor
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (7.02 mM);DMSO:62.5 mg/mL (175.38 mM)

Bioactivity

• Target IC50:
  OX1 (membrane):27 nM(Ki)|OX1 (whole cell):57 nM(Ki)
• In Vivo:
  SB-408124 (30 μg/10 μL, administered intracerebroventricularly) reduces Orexin-A-induced water intake in Wistar rats. Intracerebroventricular Orexin-A (30 μg/10 μL) inhibits vasopressin increase induced by histamine or 2.5% NaCl, and this 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).
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

selectivity, water, SB 408124, SB408124, SB-408124, intake, HCRT Receptor, Inhibitor, Hypocretin Receptor, membrane, Orexin Receptor (OX Receptor), OXReceptor, OX Receptor, OX1 (membrane), OX1 (whole cell), inhibit, cell

Compound Identifiers

PubChem CID

4331799