SB408124

Catalog No.S1545

SB408124 Chemical Structure

Molecular Weight(MW): 356.37

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.

Size Price Stock Quantity  
In DMSO USD 100 In stock
USD 70 In stock
USD 120 In stock
USD 270 In stock
USD 770 In stock
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Biological Activity

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.
Targets
OX1 (membrane) [1] OX1 (whole cell) [1]
27 nM(Ki) 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. [1] 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. [2]

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. [3] Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP). [4]

Protocol

Animal Research:

[3]

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  • Animal Models: Male Wistar rats
  • Formulation: SB-408124 is dissolved in saline.
  • Dosages: 30 μg/10 μL
  • Administration: Intracerebroventricularly (i.c.v.) injected into the lateral ventricle of the rat.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL (101.01 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.37
Formula

C19H18F2N4O

CAS No. 288150-92-5
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID