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LY255582

Catalog No. T27934   CAS 119193-09-8
Synonyms: LY-255582, LY 255582

LY255582 is a selective centrally active opioid receptor antagonist with high affinity for mu, delta and kappa receptors with Ki of 0.4 nM, 5.2, 2.0 nM, respectively. LY255582 inhibits diet-associated increases in mesolimbic dopamine levels and reduces consumption of food intake. LY255582 is commonly used in obesity research. LY255582 is a potential compound for the study of opioid receptor-mediated cell signaling.

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LY255582 Chemical Structure
LY255582, CAS 119193-09-8
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LY255582 is a selective centrally active opioid receptor antagonist with high affinity for mu, delta and kappa receptors with Ki of 0.4 nM, 5.2, 2.0 nM, respectively. LY255582 inhibits diet-associated increases in mesolimbic dopamine levels and reduces consumption of food intake. LY255582 is commonly used in obesity research. LY255582 is a potential compound for the study of opioid receptor-mediated cell signaling.
Targets&IC50 Delta:5.2 nM (Ki ), μ:0.4 nM (Ki ), κ opioid:2 nM (Ki )
In vitro LY255582 (40 μM, 24-72 h) inhibits the viability of Huh7 and MHCC-97H cells from a biological perspective.[1]
In vivo LY255582 (100 μg, i.c.v.) reduces food intake in rats [2].
LY255582 (15 mg/kg/d, s.c., once daily) decreases food intake and body weight gain in obese Zucker rats [3].
Synonyms LY-255582, LY 255582
Molecular Weight 345.52
Formula C22H35NO2
CAS No. 119193-09-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 13.5 mg/mL (39.1 mM)

TargetMolReferences and Literature

1. Levine AS, et al. Central administration of the opioid antagonist, LY255582, decreases short- and long-term food intake in rats. Brain Res. 1991;566(1-2):193-197. 2. Need AB, et al. In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously. Life Sci. 2007;81(17-18):1389-1396. 3. Gackenheimer SL, et al. Localization of opioid receptor antagonist [3H]-LY255582 binding sites in mouse brain: comparison with the distribution of mu, delta and kappa binding sites. Neuropeptides. 2005;39(6):559-567. 4. Shaw WN. Long-term treatment of obese Zucker rats with LY255582 and other appetite suppressants. Pharmacol Biochem Behav. 1993;46(3):653-659. 5. Chen DT, et al. The mu-opioid receptor is a molecular marker for poor prognosis in hepatocellular carcinoma and represents a potential therapeutic target. Br J Anaesth. 2019;122(6):157-167.

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Keywords

LY255582 119193-09-8 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor LY-255582 LY 255582 inhibitor inhibit

 

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