SB-408124- CAS 288150-92-5

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.
IC50 Value: 57 nM(Ki)
Target: OX1 Receptor
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).

Catalog Number: I002988

CAS Number: 288150-92-5

PubChem Substance ID:355201590

Molecular Formula: C19H18F2N4O

Molecular Weight:356.377

Purity: ≥95%

* For research use only. Not for human or veterinary use.




Molecular Formula: C19H18F2N4O
Molecular Weight356.377
Target:OX Receptor
SolubilityDMSO 36 mg/mL; Water <1 mg/mL
Storage3 years -20C powder
IC5057 nM(Ki)

Computed Descriptor

IUPAC Name1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea