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SB-649868

Catalog No. T5498Cas No. 380899-24-1
Alias GSK649868

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).

SB-649868

SB-649868

Purity: 99.53%
Catalog No. T5498Alias GSK649868Cas No. 380899-24-1
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 SizePriceAvailabilityQuantity
1 mg$31In Stock
5 mg$113In Stock
10 mg$197In Stock
25 mg$419In Stock
50 mg$679In Stock
100 mg$1,090In Stock
200 mg$1,460In Stock
1 mL x 10 mM (in DMSO)$138In Stock
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Purity:99.53%
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Product Introduction

Bioactivity
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
AliasGSK649868
Chemical Properties
Molecular Weight477.55
FormulaC26H24FN3O3S
Cas No.380899-24-1
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0940 mL10.4701 mL20.9402 mL104.7011 mL
5 mM0.4188 mL2.0940 mL4.1880 mL20.9402 mL
10 mM0.2094 mL1.0470 mL2.0940 mL10.4701 mL
20 mM0.1047 mL0.5235 mL1.0470 mL5.2351 mL
50 mM0.0419 mL0.2094 mL0.4188 mL2.0940 mL
100 mM0.0209 mL0.1047 mL0.2094 mL1.0470 mL

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