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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
2 mg | $68 | In Stock | |
5 mg | $118 | In Stock | |
10 mg | $190 | In Stock | |
25 mg | $313 | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $129 | 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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (122.58 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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