Almorexant HCl - 10mM in DMSO , CAS No.913358-93-7

CAS: 913358-93-7 Cat. No.: A408452 Molecular Weight: 549.02 EC Number: 695-905-6

GRADE & PURITY 10mM in DMSO

Synonyms

ACT-078573 HCl | (R)-2-((S)-1-(4-(trifluoromethyl)phenethyl)-6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide hydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Almorexant HCl (ACT-078573) is an orally active, dualorexin receptorantagonist withIC50of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.
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.

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. Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models.
Cell Data

cell lines：3T3-L1 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

ACT-078573 HCl | (R)-2-((S)-1-(4-(trifluoromethyl)phenethyl)-6, 7-dimethoxy-3, 4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide hydrochloride

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Almorexant HCl (ACT-078573) is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: CNC(=O)[C@@H](C1=CC=CC=C1)N2CCC3=CC(=C(C=C3[C@@H]2CCC4=CC=C(C=C4)C(F)(F)F)OC)OC.Cl
• Molecular Weight: 549.02
• Reaxy-Rn: 51995859
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=51995859&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 57 mg/mL (199.09 mM); Ethanol: 57 mg/mL (199.09 mM); Water: Insoluble