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SB-408124 
N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N’-[4-(dimethylamino)phenyl]urea
(CAS 288150-92-5)
Description:

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).

 

Product No. KT20318 
Product Name SB-408124 
Synonyms SB 408124; SB408124
Formal Name N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N’-[4-(dimethylamino)phenyl]urea
CAS Number 288150-92-5
Molecular Formula C19H18F2N4O
Formula Weight 356.37
Formulation A crystalline solid
Purity 98%min
Stability 2 years
Storage -20°C
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Quality Control HNMR,CNMR,LCMS,HPLC,IR,etc.
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