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SB-649868 (GSK649868) is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $197 | In Stock | |
25 mg | $419 | In Stock | |
50 mg | $679 | In Stock | |
100 mg | $1,090 | In Stock | |
200 mg | $1,460 | In Stock | |
1 mL x 10 mM (in DMSO) | $138 | In Stock |
Description | SB-649868 (GSK649868) is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively). |
Targets&IC50 | OX2:9.5 (pKi), OX1:9.4 (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 |
Alias | GSK649868 |
Molecular Weight | 477.55 |
Formula | C26H24FN3O3S |
Cas No. | 380899-24-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (209.40 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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