D159687 - PDE4D 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemED159687Cat. No.: HY-15444CAS No.: 1155877-97-6分式: CHClNO分量: 366.84作靶點: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 150 mg/mL (408.90

2、 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結(jié)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

3、儲備液可以根據(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: 2.5 mg/mL (6.81 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.81 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL

4、(6.81 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 D159687種選擇性 PDE4D 抑制劑 1。IC50 & Target PDE4D 1體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not been fully validated for medical applications.For re