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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $70 | 7-10 days | |
5 mg | $119 | 7-10 days | |
10 mg | $204 | 7-10 days | |
25 mg | $408 | 7-10 days | |
50 mg | $718 | 7-10 days | |
100 mg | $1,163 | 7-10 days | |
1 mL x 10 mM (in DMSO) | $153 | 7-10 days |
Description | Almorexant hydrochloride (ACT-078573 hydrochloride) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. |
Targets&IC50 | OX1:1.3 nM(ki), OX2:0.17 nM(ki) |
In vitro | Almorexant inhibits the increase in intracellular Ca2+ induced by 10 nM human orexin-A in Chinese hamster ovary cells with IC50 of 16 nM (rat) and 13 nM (human) for the OX1 receptor and 15 nM (rat) and 8 nM (human) for the OX2 receptor. [1] |
In vivo | Almorexant (300 mg/kg p.o.) decreases alertness, and increases electrophysiological indices of both non-REM and REM sleep in male Wistar rats. In dogs, Almorexant (100 mg/kg p.o.) causes somnolence and increases surrogate markers of REM sleep. [1] Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. [2] In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models. [3] |
Alias | ACT-078573 hydrochloride, Almorexant HCl |
Molecular Weight | 549.02 |
Formula | C29H32ClF3N2O3 |
Cas No. | 913358-93-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 48 mg/mL (87.4 mM) DMSO: 67 mg/mL (122 mM) H2O: <1 mg/mL | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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