MK-0557 - Neuropeptide Y Receptor Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMK-0557Cat. No.: HY-15411CAS No.: 328232-95-7分式: CHFNO分量: 406.41作靶點(diǎn): Neuropeptide Y Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 28 mg/mL (

2、68.90 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.4606 mL 12.3028 mL 24.6057 mL5 mM 0.4921 mL 2.4606 mL 4.9211 mL10 mM 0.2461 mL 1.2303 mL 2.4606 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 MK-0557具有度選擇性，服活性的神經(jīng)肽Y5受體拮抗劑，Ki值為

3、1.6 nM。IC50 & Target Ki: 1.6 nM (Y5) 1體外研究MK-0557 antagonizes the effects of the NPY5R-selective agonist on body-weight gain and hyperphagia inC57BL/6J mice and significantly suppresses the body-weight gain in diet-induced obese (DIO) mice. When1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemElean m

4、ice on regular chow are switched to a medium high-fat diet (4.2 kcal/g) and treated with MK-0557 at 30mg/kg PO QD, MK-0557 causes a 40% reduction inbody-weight gain at day 35 2.體內(nèi)研究 MK-0557 antagonizes the effects of the NPY5R-selective agonist on body-weight gain and hyperphagia inC57BL/6J mice and

5、 significantly suppresses the body-weight gain in diet-induced obese (DIO) mice. Whenlean mice on regular chow are switched to a medium high-fat dietREFERENCES1. Fichtner M, et al. Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor. Bioorg Med ChemLett

6、. 2012 Apr 15;22(8):2738-43.2. Erondu N, et al. Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults.Cell Metab. 2006 Oct;4(4):275-82.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820