Basic information Safety Supplier Related

LY-2940094

Basic information Safety Supplier Related

LY-2940094 Basic information

Product Name:
LY-2940094
Synonyms:
  • LY2940094;BTRX 246040;LY-2940094;LY 2940094
  • BTRX-246040
  • 2-[4-[(2'-Chloro-4',4'-difluoro-4',5'-dihydrospiro[piperidine-4,7'-[7H]thieno[2,3-c]pyran]-1-yl)methyl]-3-methyl-1H-pyrazol-1-yl]-3-pyridinemethanol
  • 3-Pyridinemethanol, 2-[4-[(2'-chloro-4',4'-difluoro-4',5'-dihydrospiro[piperidine-4,7'-[7H]thieno[2,3-c]pyran]-1-yl)methyl]-3-methyl-1H-pyrazol-1-yl]-
  • (2-(4-((2'-Chloro-4',4'-difluoro-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran]-1-yl)methyl)-3-methyl-1H-pyrazol-1-yl)pyridin-3-yl)methanol
  • depressive,orally ethanol,self-administration,Inhibitor,brain,BTRX 246040,Opioid Receptor,inhibit,penetrate,BTRX-246040,LY2940094,LY 2940094,BTRX246040,major,disorder
  • LY2940094, 10 mM in DMSO
CAS:
1307245-86-8
MF:
C22H23ClF2N4O2S
MW:
480.96
Mol File:
1307245-86-8.mol
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LY-2940094 Chemical Properties

Boiling point:
631.3±55.0 °C(Predicted)
Density 
1.51±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: 41.67 mg/mL (86.64 mM)
form 
Solid
pka
13.27±0.10(Predicted)
color 
White to yellow
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LY-2940094 Usage And Synthesis

Uses

LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models[1].

in vivo

LY2940094 (3, 10, or 30 mg/kg; 2-3 mL/kg; orally daily; for 4 days) dose-dependently reduces homecage ethanol self-administration in Indiana Alcohol-Preferring (P) and Marchigian Sardinian Alcohol-Preferring (msP) rats, without affecting food/water intake or locomotor activity[1].

Animal Model:Female Alcohol-Preferring (P) rats (250-320 g); Male Marchigian Sardinian Alcohol-Preferring (msP) rats (400-450 g)[1]
Dosage:3, 10, or 30 mg/kg; 2-3 mL/kg
Administration:Administered orally; daily; 4 days
Result:Reduced homecage ethanol self-administration.

IC 50

NOP Receptor/ORL1

References

[1] Rorick-Kehn LM, et al. A Novel, Orally Bioavailable Nociceptin Receptor Antagonist, LY2940094, Reduces Ethanol Self-Administration and Ethanol Seeking in Animal Models. Alcohol Clin Exp Res. 2016 May;40(5):945-54. DOI:10.1111/acer.13052

LY-2940094Supplier

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