LY-2940094 - Nociceptin Receptor (NOP) Antagonist - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY-2940094Cat. No.: HY-114452CAS No.: 1307245-86-8分式: CHClFNOS分量: 480.96作靶點: Opioid Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 41.67 mg/mL (86.64 m

2、M; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.0792 mL 10.3959 mL 20.7917 mL5 mM 0.4158 mL 2.0792 mL 4.1583 mL10 mM 0.2079 mL 1.0396 mL 2.0792 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備

3、液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.32 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.32 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL

4、 (4.32 mM); Suspended solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 LY-2940094種服有效的選擇性 nociceptin 受體 (NOP 受體) 拮抗劑，對 NOP 受體具有親和(Ki 為0.105 nM) 和拮抗活 (Kb=0.166 nM)。LY-2940094 可降低動物模型的給藥酒精依賴 1。IC50 & Target Ki: 0.105 nM (NOP receptor) 1Kb: 0.166 nM (NOP receptor) 1體內(nèi)研究 L

5、Y-2940094 (LY2940094; 3, 10, or 30 mg/kg; 2-3 mL/kg; orally daily; for 4 days) dose-dependently reduceshomecage ethanol self-administration in Indiana Alcohol-Preferring (P) and Marchigian Sardinian Alcohol-Preferring (msP) rats, without affecting food/water intake or locomotor activity 1.Animal Mod

6、el: Female Alcohol-Preferring (P) rats (250-320 g); Male Marchigian Sardinian Alcohol-Preferring (msP) rats (400-450 g) 1Dosage: 3, 10, or 30 mg/kg; 2-3 mL/kgAdministration: Administered orally; daily; 4 daysResult: Reduced homecage ethanol self-administration.REFERENCES1. Rorick-Kehn LM, et al. A Novel, Orally Bioavailable Nociceptin Receptor Antagonist, LY2940094, Reduces Ethanol Self-Administrationand Ethanol Seeking in Animal Models. Alcohol Clin Exp Res. 2016 May;40(5):945-54.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl