LY2795050|CAS 1346133-08-1|DC Chemicals

Cas No.:	1346133-08-1
Chemical Name:	LY2795050
Synonyms:	LY2795050
SMILES:	O=C(N)C1=CC=C(OC2=CC=C(CN3[C@H](C4=CC=CN=C4)CCC3)C=C2)C(Cl)=C1
Formula:	C₂₃N₃O₂ClH₂₂
M.Wt:	406.8934
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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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