ChemicalBook > CAS DataBase List > (R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide

(R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide

Product Name
(R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide
CAS No.
871224-64-5
Chemical Name
(R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide
Synonyms
CS-1665;Act-078573;Almorexant;AlMorexant HCl;Almorexant [inn];almorexant (ACT-078573);ACT-078573;ACT 078573;ACT078573;almorexant (ACT-078573), CID 23727689;2-(6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide;3,4-Dihydro-6,7-dimethoxy-N-methyl-alpha-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-2(1H)-isoquinolineacetamide
CBNumber
CB61512403
Molecular Formula
C29H31F3N2O3
Formula Weight
512.56
MOL File
871224-64-5.mol
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(R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide Property

Boiling point:
620.4±55.0 °C(Predicted)
Density 
1.205
storage temp. 
Desiccate at -20°C
solubility 
Soluble in DMSO
form 
Powder
pka
15.04±0.46(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
A575195
Product name
Almorexant
Packaging
5mg
Price
$120
Updated
2021/12/16
Usbiological
Product number
474055
Product name
Almorexant hcl
Packaging
100mg
Price
$1805
Updated
2021/12/16
ApexBio Technology
Product number
B3240
Product name
Almorexant
Packaging
5mg
Price
$119
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611862
Product name
Almorexant
Purity
>98%
Packaging
10mg
Price
$421.6
Updated
2021/12/16
ChemScene
Product number
CS-2484
Product name
Almorexant
Purity
99.01%
Packaging
100mg
Price
$1100
Updated
2021/12/16
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(R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide Chemical Properties,Usage,Production

Uses

Almorexant is a dual orexin receptor antagonist ACT-541468 used in the treatment of insomnia. It regulates sleep and wakefulness through two G protein-coupled receptors, namely Orexin 1 receptor and Orexin 2 receptor.

Definition

ChEBI: Almorexant is a member of isoquinolines.

Biological Activity

almorexant is an antagonist of orexin 1 receptor (ox1r) and orexin 2 receptor (ox2r) with kd values of 1.3nm and 0.17nm, respectively [1].almorexant is a dual ox antagonist. it inhibits the binding of orexin-a to both ox1r and ox2r with ic50 values of 6.6nm and 3.4nm, respectively. in the inositol phosphates assay, almorexant acts as a competitive antagonist of hox1r but a noncompetitive-like antagonist of hox2r. besides that, almorexant is found to block the increase in locomotor activity induced by icv orexin in c57bl/6 mice. furthermore, almorexant shows effects on sleep in multiple species, including man. it reduces the time spent awake and increased the time spent in nrem and rem sleep dose-dependently in normal c57bl/6 mice. these effects on sleep caused by almorexant are mediated by ox2rs as almorexant has no effect in mice lacking both ox1r and ox2r but has effects in mice lacking only ox1r [1, 2].

References

[1] malherbe p, borroni e, pinard e, wettstein jg, knoflach f. biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (ox1)/orexin 2 receptor (ox2) antagonist: comparison with selective ox1 and ox2 antagonists. mol pharmacol. 2009 sep;76(3):618-31.
[2] mang gm1, dürst t, bürki h, imobersteg s, abramowski d, schuepbach e, hoyer d, fendt m, gee ce. the dual orexin receptor antagonist almorexant induces sleep and decreases orexin-induced locomotion by blocking orexin 2 receptors. sleep. 2012 dec 1;35(12):1625-35.

(R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide Preparation Products And Raw materials

Raw materials

Preparation Products

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(R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide Suppliers

China 65 India 1 United Kingdom 1 United States 10 Global 77
Novachemistry
Tel
44-20819178-90 02081917890
Fax
(0)2080432064
Email
info@novachemistry.com
Country
United Kingdom
ProdList
4381
Advantage
58
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View Lastest Price from (R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Almorexant 871224-64-5
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Almorexant 871224-64-5
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09

871224-64-5, (R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamideRelated Search:

(R)-(+)-(3,4-Dimethoxy)benzyl-1-phenylethylamine (R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide Almorexant-13C-d3 NA Almorexant (αS,1S) Isomer Almorexant-d6

  • (R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide
  • Almorexant
  • 2-(6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide
  • (2R)-2-[(1S)-6,7-DIMETHOXY-1-[2-[4-(TRIFLUOROMETHYL)PHENYL]ETHYL]-3,4-DIHYDRO-1H-ISOQUINOLIN-2-YL]-N-METHYL-2-PHENYLACETAMIDE
  • almorexant (ACT-078573)
  • almorexant (ACT-078573), CID 23727689
  • 3,4-Dihydro-6,7-dimethoxy-N-methyl-alpha-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-2(1H)-isoquinolineacetamide
  • (2R)-2-((1S)-6,7-Dimethoxy-1-{2-(4-(trifluoromethyl)phenyl)ethyl}-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide
  • Act-078573
  • Almorexant [inn]
  • AlMorexant HCl
  • 2(1H)-IsoquinolineacetaMide,3,4-dihydro-6,7-diMethoxy-N-Methyl-a-phenyl-1-[2-[4-(trifluoroMethyl)phenyl]ethyl]-, (aR,1S)-
  • Act-078573 (R)-2-((R)-6,7-dimethoxy-1-(4-(trifluoromethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-methyl-2-phenylacetamide
  • ACT-078573;ACT 078573;ACT078573
  • CS-1665
  • 2(1H)-Isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-N-methyl-α-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-, (αR,1S)-
  • pancreatic cancer,Orexin Receptor (OX Receptor),Pancreatic ductal adenocarcinoma,Cataplexy,ACT078573,Almorexant,HCRT Receptor,Inhibitor,Apoptosis,GPCR,orexin,Hypocretin Receptor,Ca2+ channels,narcolepsy,Caspase,HPAF-II cells,AsPC-1 cells,Calcium Channel,Ca channels,hypocretin,ACT-078573,inhibit,PDAC
  • 871224-64-5
  • C29H31F3N2O3
  • Inhibitors
  • API intermediates