[CAS NO. 288150-92-5] SB-408124
PRODUCTS SPECIFICATIONS [288150-92-5]
DESCRIPTION [288150-92-5]
Overview
| MDL | MFCD06411575 |
|---|---|
| Molecular Weight | 356.37 |
| Molecular Formula | C19H18F2N4O |
| SMILES | O=C(NC1=CC(C)=NC2=C(C=C(C=C21)F)F)NC3=CC=C(C=C3)N(C)C |
Summary
SB-408124 is a non-peptide OX1 receptor antagonist with K i s of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor [1] .
IC50 & Target
|
OX 1 Receptor 57 nM (Ki, in whole cell ) |
OX 1 Receptor 27 nM (Ki, in cell membrane) |
In Vivo
SB-408124 (30 μg/10 μl; i.c.v.; male Wistar rats) decreases Orexin-A induced water intake in Wistar rats [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 140.30 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8061 mL | 14.0304 mL | 28.0607 mL |
| 5 mM | 0.5612 mL | 2.8061 mL | 5.6121 mL |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8061 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution
References
- [1] Langmead CJ, et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004;141(2):340-346.
- [2] Kis GK, et al. The osmotically and histamine-induced enhancement of the plasma vasopressin level is diminished by intracerebroventricularly administered orexin in rats. Pflugers Arch. 2012;463(4):531-536.
Synonyms