LY2795050

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY2795050 是一种新型特异性 κ-阿片受体拮抗剂 (IC50: 0.72 nM)。

LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

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.

LY2795050 (i.p., 0.032-0.1mg/kg, 30 min) prevents dose-dependent grooming deficits produced by U50,488 in male and female mice.LY2795050 (i.p., 0.032-0.1mg/kg, 0-150 min) has sexual dimorphism in some behavioral effects. Animal Model:C57BL/6J mice(gonadally intact, adult, male and female)Dosage:0.032-0.1 mg/kg Administration:i.p., 0.032-0.1mg/kg, 30 minResult:Could dose-dependently prevent the self-grooming deficits caused by U50,488 with a 30-min pre-treatment.Not effected in blocking the effects of U50,488 with smaller dose (0.032mg/kg) in either males or females.Decreased immobility in the FST in males at a dose of 0.1mg/kg, but not in females, up to a dose of 0.32mg/kg.Prevented and also reversed (at 0.32mg/kg) the locomotor-depressant effects of U50,488 (10mg/kg), in males and females.

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Endocrinology/Hormones

Opioid Receptor

κ-opioid receptor

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1346133-08-1

407.89

C23H21ClN3O2

>98% (HPLC)

DMSO:50 mg/mL (122.58 mM; Need ultrasonic)

O=C(N)C1=CC=C(OC2=CC=C(CN3[C@H](C4=CC=CN=C4)CCC3)C=C2)C(Cl)=C1

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(-20℃)

With Ice Pack

≥ 2 years