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Almorexant hydrochloride

Catalog No. T6155 CAS 913358-93-7

Synonyms: ACT-078573 hydrochloride, Almorexant HCl

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.

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Almorexant hydrochloride Chemical Structure

Almorexant hydrochloride, CAS 913358-93-7

Pack Size	Availability	Price/USD
2 mg	5 days	$ 70.00
5 mg	5 days	$ 119.00
10 mg	5 days	$ 204.00
25 mg	5 days	$ 408.00
50 mg	5 days	$ 718.00
100 mg	5 days	$ 1,163.00
1 mL * 10 mM (in DMSO)	5 days	$ 153.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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	OX2:0.17 nM(ki), OX1:1.3 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]

Synonyms	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

Solubility Information

Ethanol: 48 mg/mL (87.4 mM)

DMSO: 67 mg/mL (122 mM)

H2O: <1 mg/mL

References and Literature

1. Brisbare-Roch C, et al. Nat Med. 2007, 13(2), 150-155. 2. Nollet M, et al. Neuropsychopharmacology. 2012, 37(10), 2210-2221. 3. Anderson RI, et al. Front Neurosci. 2014, 8, 33.

Related Products

Related compounds with same targets

MK-1064 Orexin 2 Receptor Agonist SB-408124 Almorexant EMPA DORA-22 MK-3697 Seltorexant

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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