LY2795050
Modify Date: 2024-01-09 20:36:06
LY2795050 structure
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Common Name | LY2795050 | ||
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| CAS Number | 1346133-08-1 | Molecular Weight | 407.89300 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H22ClN3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of LY2795050LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1]Target: κ-opioid Receptorin vitro: LY2795050 displays full antagonist activity and high binding affinity and selectivity for KOR with a ki value of 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 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]. |
| Name | 3-chloro-4-[4-[ [ (2S)-2-(3-pyridyl)pyrrolidin-1-yl]methyl]phenoxy]benzamide |
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| Synonym | More Synonyms |
| Description | LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1]Target: κ-opioid Receptorin vitro: LY2795050 displays full antagonist activity and high binding affinity and selectivity for KOR with a ki value of 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 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]. |
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| Related Catalog | |
| References |
| Molecular Formula | C23H22ClN3O2 |
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| Molecular Weight | 407.89300 |
| Exact Mass | 407.14000 |
| PSA | 68.45000 |
| LogP | 5.60150 |
| Storage condition | 2-8℃ |
| LY2795050 |