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SB-408124 is a non-peptide antagonist selective for the orexin receptor subtype OX1, with around 70-fold selectivity for OX1 over OX2 receptors, and improved oral bioavailability compared to the older OX1 antagonist SB-334,867. It is used in scientific research into the function of orexinergic neurons in the body.
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| Cell lines | |
| Preparation method | |
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| Incubation time | |
| Animal Experiment | |
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| Animal models | Male Wistar rats |
| Formulation | SB-408124 is dissolved in saline. |
| Dosages | 30 μg/10 μL |
| Administration | Intracerebroventricularly (i.c.v.) injected into the lateral ventricle of the rat. |
| Molecular Weight | 356.37 |
| Formula | C19H18F2N4O |
| CAS Number | 288150-92-5 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related OX Receptor Products |
|---|
| MK-6096
MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R. |
| Almorexant
Almorexant is a competitive OX1 and OX2 orexin receptor antagonist with IC50 of 13 and 8 nM, respectively. |
| MK-3697
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM. |
| TCS-1102
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). |
| SB-334867 hydrochloride
SB-334867 hydrochloride is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. |
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