[CAS NO. 1431697-90-3] SB-408124Hydrochloride
PRODUCTS SPECIFICATIONS [1431697-90-3]
DESCRIPTION [1431697-90-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 392.83 |
| Molecular Formula | C19H19ClF2N4O |
| SMILES | O=C(NC1=CC=C(C=C1)N(C)C)NC2=CC(C)=NC(C2=CC(F)=C3)=C3F.[H]Cl |
Summary
SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with K i s of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride 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 Vitro
Primary neuronal cultures from the hypothalamus of newborn SD rats are incubated with orexin A (1 µM), orexin A (1 µM) together with SB-408124 (100 µM) for 6 h. Orexin A-induced increases in arginine vasopressin (AVP) mRNA levels (2.7-fold) are attenuated by SB-408124 (1.2-fold) [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SB-408124 reduces anxiety after psychotraumatic exposure. Predator induces acute psychotraumatic exposure decrease corticoliberin level in the rat's amygdala. Intranasal administration of SB-408124 restores it closely to normal and has an anxiolytic effect on animal behaviour
[2]
.
Bilateral paraventricular nucleus microinjection of SB-408124 (30 pmol/50 nL per side) results in a greater reduction in mean arterial pressure (MAP) in high-salt intake (-16 mmHg) compared with NS-fed (-4 mmHg) anesthetized Dahl salt-sensitive rats
[3]
.
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
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 1 mg/mL ( 2.55 mM ; ultrasonic and warming and heat to 60°C)
DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5456 mL | 12.7282 mL | 25.4563 mL |
| 5 mM | --- | --- | --- |
| 10 mM | --- | --- | --- |
References
- [1] Langmead et al (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br.J.Pharmacol. 141 340.
- [2] I Tissen, et al. OX1R ANTAGONIST SB408124 ACTION AND EXTRAHYPOTHALAMIC CRF IN RATS AFTER PSYCHOTRAUMATIC EXPOSURE. Georgian Med News. 2019 May;(290):127-131.
- [3] Michael J Huber, et al. Increased activity of the orexin system in the paraventricular nucleus contributes to salt-sensitive hypertension. Am J Physiol Heart Circ Physiol. 2017 Dec 1;313(6):H1075-H1086.
Synonyms