1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. SB-408124 Hydrochloride

SB-408124 Hydrochloride 

Cat. No.: HY-76612 Purity: 98.09%
Handling Instructions

SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor.

For research use only. We do not sell to patients.

SB-408124 Hydrochloride Chemical Structure

SB-408124 Hydrochloride Chemical Structure

CAS No. : 1431697-90-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 336 In-stock
Estimated Time of Arrival: December 31
100 mg USD 600 In-stock
Estimated Time of Arrival: December 31
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Description

SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis 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[1]

OX1 Receptor

57 nM (Ki, in whole cell )

OX1 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.

Molecular Weight

392.83

Formula

C₁₉H₁₉ClF₂N₄O

CAS No.

1431697-90-3

SMILES

O=C(NC1=CC=C(C=C1)N(C)C)NC2=CC(C)=NC(C2=CC(F)=C3)=C3F.[H]Cl

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
References
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Keywords:

SB-408124SB408124SB 408124Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorOX1non-peptidevasopressinInhibitorinhibitorinhibit

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Product Name:
SB-408124 Hydrochloride
Cat. No.:
HY-76612
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