product name SB408124
Description: SB408124 is a potent, novel, selective, non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, it exhibits 50-fold selectivity over OX2 receptor. Pre-treated with SB408124 before orexin A in primary astrocyte cultures from the rat cerebral cortex remarkably decreased the orexin A stimulatory activity on forskolin and basal-induced cAMP production.
References: Br J Pharmacol. 2004 Jan;141(2):340-6.; Pharmacol Rep. 2011;63(3):717-23; Pflugers Arch. 2012 Apr;463(4):531-6.
356.37
Formula
C19H18F2N4O
CAS No.
288150-92-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 36 mg/mL (101.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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). |
| Animal model | Male Wistar rats |
| Formulation & Dosage | Dissolved in saline; 30 μg/10 μL; Intracerebroventricularly (i.c.v.) injected into the lateral ventricle of the rat. |
| References | Br J Pharmacol. 2004 Jan;141(2):340-6.; Pharmacol Rep. 2011;63(3):717-23; Pflugers Arch. 2012 Apr;463(4):531-6. |
