Home GPCR & G Protein OX Receptor antagonist SB408124 For research use only.

SB408124

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.

SB408124 Chemical Structure

SB408124 Chemical Structure

CAS: 288150-92-5

Selleck's SB408124 has been cited by 1 publication

Purity & Quality Control

Batch: S154501 DMSO] 36 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.74%
99.74

SB408124 Related Products

Signaling Pathway

OX Receptor Signaling Pathways

OX Receptor Signaling Pathway

Choose Selective OX Receptor Inhibitors

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
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
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]
Animal Research Animal Models Male Wistar rats
Dosages 30 μg/10 μL
Administration Intracerebroventricularly (i.c.v.) injected into the lateral ventricle of the rat.

Chemical Information & Solubility

Molecular Weight 356.37 Formula

C19H18F2N4O
CAS No. 288150-92-5 SDF Download SB408124 SDF
Smiles CC1=CC(=C2C=C(C=C(C2=N1)F)F)NC(=O)NC3=CC=C(C=C3)N(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 36 mg/mL ( (101.01 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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