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SB-408124

Catalog No. T6658 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.

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SB-408124, CAS 288150-92-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 180.00
50 mg	In stock	$ 323.00
100 mg	In stock	$ 479.00
1 mL * 10 mM (in DMSO)	In stock	$ 59.00

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Purity: 98.14%

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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&IC50	OX1 (whole cell):57 nM(Ki), OX1 (membrane):27 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]

Molecular Weight	356.37
Formula	C19H18F2N4O
CAS No.	288150-92-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35.6 mg/mL (100 mM)

References and Literature

1. Langmead CJ, et al, Br J Pharmacol, 2004, 141(2) , 340-346. 2. Woldan-Tambor A, et al, Pharmacol Rep, 2011, 63(3), 717-723. 3. Kis Gk, et al, Pflugers Arch, 2012, 463(4), 531-536 4. Yi CX, et al, Diabetes, 2009, 58(9), 11998-22005.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Membrane Protein-targeted Compound Library Covalent Inhibitor Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Bioactive Compound Library

Related Products

Related compounds with same targets

MK-1064 Almorexant YNT-185 EMPA IPSU Daridorexant hydrochloride MK-3697 Almorexant hydrochloride

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Keywords

SB-408124 288150-92-5 GPCR/G Protein Neuroscience OX Receptor inhibit water membrane selectivity Inhibitor Orexin Receptor (OX Receptor) intake Hypocretin Receptor HCRT Receptor SB 408124 cell SB408124 inhibitor

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