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LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $48 | In Stock | In Stock | |
| 2 mg | $68 | In Stock | In Stock | |
| 5 mg | $118 | In Stock | In Stock | |
| 10 mg | $190 | In Stock | In Stock | |
| 25 mg | $313 | In Stock | In Stock | |
| 50 mg | Preferential | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $129 | In Stock | In Stock |
| Description | LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM). |
| Targets&IC50 | κ opioid receptor:0.72 nM |
| In vitro | LY2795050 displays full antagonist activity and high binding affinity and selectivity for κ-opioid Receptor (Ki: 0.72 nM) [1]. |
| In vivo | In the brain, (11)C-LY2795050 displayed fast uptake kinetics (regional activity peak times of <20 min) and an uptake pattern consistent with the distribution of κ-Opioid Receptor (KOR) in primates [1]. The LY2795050 ED50 at MOR was 119 μg/kg based on a 1-site model for 11C-carfentanil. The 1-site binding model was also deemed sufficient to describe the specific binding of 11C-LY2795050 at KOR. The ED50 at KOR estimated from the 1-site model was 15.6 μg/kg. Thus, the ED50 ratio for MOR:KOR was 7.6 [2]. |
| Molecular Weight | 407.89 |
| Formula | C23H22ClN3O2 |
| Cas No. | 1346133-08-1 |
| Smiles | NC(=O)c1ccc(Oc2ccc(CN3CCC[C@H]3c3cccnc3)cc2)c(Cl)c1 |
| Relative Density. | 1.287 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (122.58 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.9 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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