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SB-649868

SKU: orb1301739

Description

SB-649868 (GSK649868) is a potent, selective, and orally bioavailable dual orexin receptor antagonist, exhibiting high affinity for both OX1 and OX2 receptors. It is a valuable research tool for investigating sleep-wake regulation, stress responses, and addiction pathways in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number380899-24-1
MW477.55
Purity99.58% (May vary between batches)
FormulaC26H24FN3O3S
SMILESCc1nc(C(=O)N2CCCC[C@H]2CNC(=O)c2cccc3occc23)c(s1)-c1ccc(F)cc1
TargetOX Receptor
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.38 mM);DMSO:100 mg/mL (209.4 mM)

Bioactivity

Target IC50
OX1:9.4 (pKi)|OX2:9.5 (pKi)
In Vitro
SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pKb values are 9.67 0.03 and 9.64 0.07 for OX1 and OX2

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

OXReceptor, SB649868, SB-649868, SB 649868, inhibit, Inhibitor, OX Receptor, OX1, OX2, Orexin Receptor (OX Receptor), GSK 649868, GSK649868, GSK-649868, HCRT Receptor, Hypocretin Receptor

Similar Products

  • SB-649868 [orb1225149]

    >98% (HPLC)

    380899-24-1

    477.554

    C26H24FN3O3S

    5 mg, 10 mg, 100 mg, 200 mg, 500 mg, 1 g, 50 mg, 25 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

Protocol Information

Available Sizes

Select a size below

5 mg
$ 110.00
1 ml x 10 mM (in DMSO)
$ 130.00
10 mg
$ 160.00
25 mg
$ 300.00
50 mg
$ 450.00
100 mg
$ 700.00
200 mg
$ 920.00
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