LY2795050

Short Summary : KOR antagonist

Category : Endocrinology and Hormones|Opioid Receptor

Purity : 0.98

CAS Number : 1346133-08-1

Formula : C23H22ClN3O2

Molecular Weight : 407.89

SMILE : O=C(N)C(C=C1)=CC(Cl)=C1OC(C=C2)=CC=C2CN3C(C4=CN=CC=C4)CCC3

Solubility : 25℃: DMSO

Storage : Store at -20°C

Description : Description:
IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1]
LY2795050 is a novel selective KOR antagonist and has the potential as a PET tracer to image KOR in vivo.
in 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].
Clinical trial: N/A

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