Almorexant HCl

Catalog No.S2160 Synonyms: ACT-078573 HCl

For research use only.

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.

Almorexant HCl Chemical Structure

CAS No. 913358-93-7

Selleck's Almorexant HCl has been cited by 3 Publications

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Purity & Quality Control

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Biological Activity

Description 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.
Features Orally bioavailable orexin receptor antagonist that has been tested in Phase III clinical trials for treatment of Insomnia.
Targets
OX2 receptor [1] OX1 receptor [1]
3.4 nM 6.6 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO NXj5bXBvTnWwY4Tpc44h[XO|YYm= M3HT[FMxKG2rboO= M1\xS2Rqe3CuYXPlcYVvfCCxZjDbNVI2UV1vT4LlfIlvKEFiZoLvcUBpfW2jbjDPXFJTKGW6cILld5Nm\CCrbjDDTG8h[2WubIOgZYZ1\XJiM{CgcYlveyCkeTD0c5Bkd3WwdDDhcoFtgXOrczygT4khRSByLkCwOFch|ryPLh?= M3;5V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[3NFA1Lz5{NUK2O|AxPDxxYU6=
CHO NIr5RlNHfW6ldHnvckBie3OjeR?= M3HmVWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hV1h{UjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhd3KneHnuMWEucW6mdXPl[EBqdnS{YXPlcIx2dGG{IHPhcINqfW1icnXs[YF{\SxiSVO1NEA:KDBwMEC4JO69VS5? MmrQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|MUe1PVEoRjJ4M{G3OVkyRC:jPh?=
CHO M2\LcmZ2dmO2aX;uJIF{e2G7 M{fEXGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hV1h{UjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2GuY3n1cUBud2KrbHn6ZZRqd25iYomgSmxKWFJiYYPzZZktKEmFNUCgQUAxNjByODFOwG0v MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzOUKzNUc,OjN5MUmyN|E9N2F-
CHO MWXGeY5kfGmxbjDhd5NigQ>? MmLGRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBQYDGUIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBwemW6aX6tRU1qdmS3Y3XkJIlvfHKjY3XscJVt[XJiY3HsZ4l2dSC{ZXzlZZNmNCCLQ{WwJF0hOC5yMUOg{txONg>? NFPUUJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkOxO|U6OSd-Mk[zNVc2QTF:L3G+
CHO NGP0Z3JHfW6ldHnvckBie3OjeR?= M2L3W2FvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hV1hzUjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2GuY3n1cUBud2KrbHn6ZZRqd25iYomgSmxKWFJiYYPzZZktKEmFNUCgQUAxNjBzMzFOwG0v MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzOUKzNUc,OjN5MUmyN|E9N2F-
Assay
Methods Test Index PMID
Western blot PhosphoTyr / SHP2 29467942
Growth inhibition assay Tumor volume 29467942
IHC H&E staining ; OX1R / Activated caspase-3 26943473 29467942
Immunofluorescence NPY / ORX-A ; BDNF / NPY 27727245 32066707
Representative autoradiograms LC / TMN / DRN 22768296
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]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Wistar rats.
  • Dosages: ~300 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+25% β-cyclodextrin in saline
For best results, use promptly after mixing.

9mg/mL

Chemical Information

Molecular Weight 549.02
Formula

C29H32ClF3N2O3

CAS No. 913358-93-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNC(=O)C(C1=CC=CC=C1)N2CCC3=CC(=C(C=C3C2CCC4=CC=C(C=C4)C(F)(F)F)OC)OC.Cl

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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