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GPCR/G Protein OX Receptor SB408124

SB408124

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.

SB408124, CAS 288150-92-5
Pack Size Availability Price/USD Quantity
5 mg Inquiry 50.00
10 mg Inquiry 90.00
25 mg Inquiry 200.00
50 mg Inquiry 360.00
100 mg Inquiry 690.00
1 mL * 10 mM (in DMSO) Inquiry 51.00
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Purity 98.0%
Biological Description
Chemical Properties
Storage & Solubility Information
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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 (membrane) : 27nM(Ki),   OX1 (whole cell) : 57nM(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]
Animal Research
Animal Model: Wistar rats
Molecular Weight 356.37
Formula C19H18F2N4O
CAS No. 288150-92-5

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 35.6 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL

Citations

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.

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