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GPCR/G Protein OX Receptor Almorexant HCl

Almorexant HCl

Catalog No. T6155   CAS 913358-93-7
Synonyms: ACT-078573 hydrochloride, Almorexant hydrochloride, Almorexant hydrochloride, ACT-078573 hydrochloride

Almorexant HCl (ACT078573) 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.

Almorexant HCl, CAS 913358-93-7
Pack Size Availability Price/USD Quantity
2 mg Inquiry 78.00
5 mg Inquiry 133.00
10 mg Inquiry 227.00
25 mg Inquiry 454.00
50 mg Inquiry 798.00
100 mg Inquiry 1293.00
1 mL * 10 mM (in DMSO) Inquiry 170.00
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Purity 98.0%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description Almorexant HCl (ACT078573) 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 : ic50 6.6nM,   OX2 : ic50 3.4nM,  
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]
Animal Research
Animal Model: Wistar rats.
Synonyms ACT-078573 hydrochloride , Almorexant hydrochloride , Almorexant hydrochloride , ACT-078573 hydrochloride
Purity 98.0%
Molecular Weight 549.02
Formula C29H32ClF3N2O3
CAS No. 913358-93-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 67 mg/mL (122 mM)

Ethanol: 48 mg/mL (87.4 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

2% DMSO/25% β-cyclodextrin/saline: 9mg/mL

Citations

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. 4. Borniger JC, et al. A Role for Hypocretin/Orexin in Metabolic and Sleep Abnormalities in a Mouse Model of Non-metastatic Breast Cancer. Cell Metab. 2018 Jul 3;28(1):118-129.e5.

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Nitroaspirin Lemborexant MK1064 PF3274167 Aloin TCS 1102 Almorexant MK3697

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