D159687 - PDE4D 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemED159687Cat. No.: HY-15444CAS No.: 1155877-97-6分式: CHClNO分量: 366.84作靶点: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (408.90

2、 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7260 mL 13.6299 mL 27.2598 mL5 mM 0.5452 mL 2.7260 mL 5.4520 mL10 mM 0.2726 mL 1.3630 mL 2.7260 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；澄清的

3、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: 2.5 mg/mL (6.81 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.81 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL

4、(6.81 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 D159687种选择性 PDE4D 抑制剂 1。IC50 & Target PDE4D 1体外研究 D159687 (1 M, 0-24hours) induces a transient increase in CREB phosphorylation which peaked at 6hoursafter treatment 1.D159687 (0.01-1 M, 6 hours) causes

5、optimal CREB phosphorylation at 1M 1.Western Blot Analysis 1Cell Line: HT-22 (mouse hippocampal cell line)Concentration: 1 MIncubation Time: 0, 1, 3, 6, 12, 24hoursResult: Induced a transient increase in CREB phosphorylation which peaked at 6hours aftertreatment.Western Blot Analysis 1Cell Line: HT-

6、22 (mouse hippocampal cell line)Concentration: 0.01 M, 0.1 M, 1 MIncubation Time: 6 hoursResult: CREB phosphorylation was optimal at 1M.体内研究 D159687 (0.05-5 mg/kg; oral daily for a week) shows a potential recruitment or enhancement of synapticfunction with increased task difficulty in female Cynomol

7、gus macaques 2.Animal Model: Female Cynomolgus macaques (46 year old) 2Dosage: 0.05, 0.5, 5 mg/kgAdministration: Oral daily for a weekResult: A potential recruitment or enhancement of synaptic function with increased task difficulty.REFERENCES1. Zhang C, et al. Comparison of the Pharmacological Profiles of Selective PDE4B and PDE4D Inhibitors in the Central Nervous System.Sci Rep. 2017 Jan 5;7:40115.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCaution: Product has not been fully validated for medical applications.For re