LY255582
Based on 1 Customer Validation
LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity.
For research use only. We do not sell to patients.
- Purity : 98%
- CAS No.: 119193-09-8
- Formula: C22H35NO2
- Molecular Weight:345.52
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Storage:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
All Opioid Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
μ Opioid Receptor/MOR 0.4 nM (Ki) |
δ Opioid Receptor/DOR 5.2 nM (Ki) |
κ Opioid Receptor/KOR 2.0 nM (Ki) |
In Vitro
LY255582 (40 μM, 24-72 h) reduces cell viability of Huh7 and MHCC-97H cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
LY255582 (15 mg/kg, s.c., once daily) decreases food intake and body weight gain of fed obese Zucker rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:STZ-induced diabetic mice[1]
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Dosage:100, 10 and 1 μg
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Administration:i.c.v.
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Result:Decreased food at 100, 10 and 1 μg by 76, 62 and 29%.
Chemical Information
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CAS No. 119193-09-8
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Appearance Solid
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Molecular Weight 345.52
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Formula C22H35NO2
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Color White to off-white
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SMILES
OC1=CC([C@]2([C@H](CN(CC2)CC[C@@H](C3CCCCC3)O)C)C)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 15 mg/mL (43.41 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Levine AS, et al. Central administration of the opioid antagonist, LY255582, decreases short- and long-term food intake in rats. Brain Res. 1991 Dec 6;566(1-2):193-7. [Content Brief]
[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 Oct 13;81(17-18):1389-96. [Content Brief]
[4]. Shaw WN, et al. Long-term treatment of obese Zucker rats with LY255582 and other appetite suppressants. Pharmacol Biochem Behav. 1993 Nov;46(3):653-9. [Content Brief]
[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 Jun;122(6):e157-e167. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8942 mL | 14.4709 mL | 28.9419 mL | 72.3547 mL |
| 5 mM | 0.5788 mL | 2.8942 mL | 5.7884 mL | 14.4709 mL | |
| 10 mM | 0.2894 mL | 1.4471 mL | 2.8942 mL | 7.2355 mL | |
| 15 mM | 0.1929 mL | 0.9647 mL | 1.9295 mL | 4.8236 mL | |
| 20 mM | 0.1447 mL | 0.7235 mL | 1.4471 mL | 3.6177 mL | |
| 25 mM | 0.1158 mL | 0.5788 mL | 1.1577 mL | 2.8942 mL | |
| 30 mM | 0.0965 mL | 0.4824 mL | 0.9647 mL | 2.4118 mL | |
| 40 mM | 0.0724 mL | 0.3618 mL | 0.7235 mL | 1.8089 mL |