LY2795050_product_DataBase

Bioactivity

LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction[1][2].

Target

Ki: 0.72 nM (KOR); Kb: 0.63 nM (KOR)

Invitro

LY2795050 displays high affinity with a Ki value of 0.72 nM for the KOR and has antagonist activity with a Kb value of 0.63 nM[1].

In Vivo

LY2795050 (i.p., 0.032-0.1mg/kg, 30 min) prevents dose-dependent grooming deficits produced by U50,488 in male and female mice[2].LY2795050 (i.p., 0.032-0.1mg/kg, 0-150 min) has sexual dimorphism in some behavioral effects[2]. Animal Model:

Name

LY2795050

CAS

1346133-08-1

Formula

C23H22ClN3O2

Molar Mass

407.89

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Ming-Qiang Zheng, et al. Synthesis and evaluation of 11C-LY2795050 as a κ-opioid receptor antagonist radiotracer for PET imaging. J Nucl Med [2]. Eduardo R Butelman, et al. Profile of a short-acting κ-antagonist, LY2795050, on self-grooming behaviors, forced swim test and locomotor activity: sex comparison in mice. J Psychopharmacol. 2021 May;35(5):579-590.

PeptideDB

LY2795050

CAS: 1346133-08-1 F: C23H22ClN3O2 W: 407.89