GSK-256066-Trifluoroacetate-GSK256066-2-2-2-trifluoroacetic-acid-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK 256066 TrifluoroacetateCat. No.: HY-70069CAS No.: 1415560-64-3Synonyms: GSK256066 (2,2,2-trifluoroacetic acid)分式: CHFNOS分量: 632.61作靶點: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn

2、 solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (79.04 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.5808 mL 7.9038 mL 15.8075 mL5 mM 0.3162 mL 1.5808 mL 3.1615 mL10 mM 0.1581 mL 0.7904 mL 1.5808 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

3、擇適當(dāng)?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(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)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: 3.25 mg/mL (5.14 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.25 mg/mL (5.14 mM); Clea

4、r solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 GSK 256066 Trifluoroacetate種選擇性、親和的 PDE 抑制劑，抑制 PDE4B 的 IC50 值為 3.2 pM。被開發(fā)于治療慢性阻塞性肺病 1。IC50 & Target IC50: 3.2 pM (PDE4B) 1體外研究 GSK 256066 Trifluoroacetate is an exceptionally high-affinity inhibitor of PDE4 designed fo

5、r inhaledadministration 1.GSK 256066 Trifluoroacetate is highly selective for PDE4, with 380,000-fold versus PDE1/2/3/5/6 and2500-fold against PDE7, and inhibits PDE4 isoforms A-D with equal affinity 1.GSK 256066 Trifluoroacetate inhibits tumor necrosis factor production by lipopolysaccharide (LPS)-

6、stimulated human peripheral blood monocytes with IC50 of 0.01 nM 1.體內(nèi)研究 GSK 256066 Trifluoroacetate (0.3-100 g/kg; intratracheally) inhibits the eosinophil number increased in thebronchoalveolar lavage (BAL) in a dose-dependent fashion, in lipopolysaccharide (LPS)- and ovalbumin(OVA)-induced acute p

7、ulmonary inflammation rat models. 2.GSK 256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes areobserved in ferrets 2.Animal Model: Male Brown Norway rats(180-200 g) 2Dosage: 0.3-100 g/kgAdministration: Intratracheally; 30 minutes before and 6 hours after ovalb

8、umin challengeResult: Inhibited the increase in eosinophil number in the BAL in a dose-dependent fashion.REFERENCES1. Tralau-Stewart CJ, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable foradministration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther, 2011, 337(1), 145-154.2. Nials AT, et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther,2011, 337(1), 137-144.McePdfHeightCaution: Product has not been fully validated for medical a