ChemicalBook > CAS DataBase List > ACT-462206

ACT-462206

Product Name
ACT-462206
CAS No.
1361321-96-1
Chemical Name
ACT-462206
Synonyms
ACT-462206;ACT 462206,ACT462206;ACT-462206 >=98% (HPLC);ACT-462206, 10 mM in DMSO;(2S)-N-(3,5-DIMETHYLPHENYL)-1-(4-METHOXYPHENYL)SULFONYLPYRROLIDINE-2-CARBOXAMIDE;(2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide;2-Pyrrolidinecarboxamide, N-(3,5-dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-, (2S)-
CBNumber
CB53167703
Molecular Formula
C20H24N2O4S
Formula Weight
388.48
MOL File
1361321-96-1.mol
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ACT-462206 Property

Density 
1.285±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
pka
14.27±0.70(Predicted)
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1393
Product name
ACT-462206
Purity
≥98% (HPLC)
Packaging
5 mg
Price
$86.92
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1393
Product name
ACT-462206
Purity
≥98% (HPLC)
Packaging
25 mg
Price
$272
Updated
2025/07/31
Tocris
Product number
5319
Product name
ACT462206
Purity
≥99%(HPLC)
Packaging
10
Price
$219
Updated
2021/12/16
Tocris
Product number
5319
Product name
ACT462206
Purity
≥99%(HPLC)
Packaging
50
Price
$815
Updated
2021/12/16
TRC
Product number
A305313
Product name
ACT462206
Packaging
2.5mg
Price
$220
Updated
2021/12/16
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ACT-462206 Chemical Properties,Usage,Production

Uses

ACT-462206 is a potent and selective dual orexin receptor antagonist (DORA) that inhibits the stimulating effects of the orexin peptides at both the orexin 1 and 2 receptors. It decreases wakefulness and increases non-rapid eye movement (non-REM) and REM sleep while maintaining natural sleep architectures in some animal models while showing anxiolytic-like properties without affecting cognition and motor function in others.

Biological Activity

ACT-462206 is a orally active, brain penetrant, potent and selective dual orexin1/2 receptor antagonist (DORA). ACT-462206 decreases wakefulness, decreases sleep latency, and increases sleep efficacy in rats and dogs.', 'ACT-462206 is a proline sulphonamide with the potential to tre at insomnia. On absorption, its displays asthenia, blurred vision, and fatigue as adverse events.

in vivo

ACT-462206 (compound 24) (100 mg/kg; p.o.; sampling at 3 h) can go cross blood brain barrier, with concentrations are 2267 ng/mL and 1219 ng/g in plasma and brain, respectively in male Wistar rats[1].
ACT-462206 (10-300 mg/kg; p.o.; single dose) shows sleep-promoting effects in male Wistar rats and in male Beagle dogs, with decreasing wakefulness and increasing non-rapid eye movement (non-REM) and REM sleep[1].
ACT-462206 (100, 300 mg/kg; p.o.; single dose) exerts anxiolytic-like effects, decreases the fear-potentiated startle reflexes in response to a sudden loud noise in rats, reduces the socialstress-induced increases of locomotion, body temperature, and heart rate[1].
Pharmacokinetics in different species[1]

RouteDose (mg/kg)AUC (ng h/mL)CL (mL/min/kg)Vss (L/kg)t1/2 (h)cmax (ng/mL)tmax (h)F1/2 (%)
rati.v.1586291.81.9///
p.o.102310///16000.539
dogi.v.11490111.41.7///
p.o.32750///4260.552
Animal Model:Male Wistar rats[1]
Dosage:0, 10, 30, 100, 300 mg/kg
Administration:Oral gavage; single dose
Result:Decreased the latency to the first persistent episode of non-REM sleep (60 s) and the first persistent episode of REM sleep (30 s).
Dose-dependently decreased total wake time and behavioral home cage activity (one-way ANOVA; p <0.001), while increasing REM and non-REM sleep times.

IC 50

OX2; OX1

storage

Store at +4°C

ACT-462206 Preparation Products And Raw materials

Raw materials

Preparation Products

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ACT-462206 Suppliers

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1361321-96-1, ACT-462206Related Search:


  • ACT-462206
  • (2S)-N-(3,5-DIMETHYLPHENYL)-1-(4-METHOXYPHENYL)SULFONYLPYRROLIDINE-2-CARBOXAMIDE
  • (2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide
  • ACT-462206 >=98% (HPLC)
  • ACT 462206,ACT462206
  • 2-Pyrrolidinecarboxamide, N-(3,5-dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-, (2S)-
  • ACT-462206, 10 mM in DMSO
  • 1361321-96-1