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LY2940094

Cat. No. M10510
LY2940094 Structure
Synonym:

BTRX-246040; LY-2940094

Size Price Availability
5mg USD 220  USD220 4-7 Days
10mg USD 360  USD360 4-7 Days
25mg USD 700  USD700 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LY-2940094 is a potent, selective and orally available antagonist of nociceptin receptor (NOP receptor) with Ki of 0.105 nM and Kb of 0.166 nM. 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. LY-2940094 reduces ethanol self-administration in animal models. Furthermore, LY2940094 blocked ethanol-stimulated dopamine release in response to ethanol challenge (1.1 g/kg, IP).

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Female Alcohol-Preferring (P) rats (250-320 g); Male Marchigian Sardinian Alcohol-Preferring (msP) rats (400-450 g)
Formulation dissolved in 20% Captisol in 25 mM phosphate buffer (pH 3, adjusted for L-tartaric acid salt weight)
Dosages 3, 10, or 30 mg/kg; 2-3 mL/kg
Administration 4 daily orally administered
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 480.96
Formula C22H23ClF2N4O2S
CAS Number 1307245-86-8
Purity >99%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

[1] Linda M Rorick-Kehn, et al. Alcohol Clin Exp Res. A Novel, Orally Bioavailable Nociceptin Receptor Antagonist, LY2940094, Reduces Ethanol Self-Administration and Ethanol Seeking in Animal Models

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Keywords: LY2940094, BTRX-246040; LY-2940094 supplier, Opioid Receptor, inhibitors

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