PQ-912-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPQ-912Cat. No.: HY-123821CAS No.: 1276021-65-8分式: CHNO分量: 336.39作靶点: Amyloid-作通路: Neuronal Signaling储存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性数据体外实验 DMSO : 200 mg/mL (594

2、.55 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9727 mL 14.8637 mL 29.7274 mL5 mM 0.5945 mL 2.9727 mL 5.9455 mL10 mM 0.2973 mL 1.4864 mL 2.9727 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；

3、澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 5 mg/mL (14.86 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 5 mg/mL (14.86 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 5 mg/mL (

4、14.86 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 PQ-912氨酰胺环化酶 (QC) 的竞争性抑制剂 1。PQ-912 抑制、和的氨酰胺环化酶活性，其Ki 值在 20-65 nM 之间 2。IC50 & Target Ki: 25 nM (human glutaminyl cyclase, pH:8.0); 65 nM (Mouse glutaminyl cyclase; pH:8.0) 2体内研究 PQ-912 (oral treatment; 20

5、0 mg/kg/day for 1 week in hAPPSLxhQC double-transgenic mice) shows asignificant reduction of pE-A levels 2.Animal Model: hAPPSLxhQC double-transgenic mice 2Dosage: 200 mg/kgAdministration: Oral treatment; daily for 1 weekResult: Showed a significant reduction of pE-A levels.REFERENCES1. Lues I, et a

6、l. A phase 1 study to evaluate the safety and pharmacokinetics of PQ912, a glutaminyl cyclase inhibitor, in healthy subjects.Alzheimers Dement (N Y). 2015 Oct 3;1(3):182-195.2. Hoffmann T, et al. Glutaminyl Cyclase Inhibitor PQ912 Improves Cognition in Mouse Models of Alzheimers Disease-Studies on Relationto Effective Target Occupancy. J Pharmacol Exp Ther. 2017 Jul;362(1):119-130.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel