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GSK256066 Trifluoroacetate

CAS number:1415560-64-3    molecular formula:C29H27F3N4O7S

overview

compound introduction

GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC 50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease In Vitro GSK256066 Trifluoroacetate is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration. GSK256066 Trifluoroacetate is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7, and inhibits PDE4 isoforms A-D with equal affinity. GSK256066 Trifluoroacetate inhibits tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC 50 of 0.01 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GSK256066 Trifluoroacetate (0.3-100 μg/kg; intratracheally) inhibits the eosinophil number increased in the bronchoalveolar lavage (BAL) in a dose-dependent fashion, in lipopolysaccharide (LPS)- and ovalbumin (OVA)-induced acute pulmonary inflammation rat models.. GSK256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes are observed in ferrets. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Brown Norway rats(180-200 g)Dosage: 0.3-100 μg/kg Administration: Intratracheally; 30 minutes before and 6 hours after ovalbumin challenge Result: Inhibited the increase in eosinophil number in the BAL in a dose-dependent fashion. Form:Solid IC50& Target:IC50: 3.2 pM (PDE4B)

Specs

Chinese aliasGSK256066 三氟乙酸盐
English aliasAKOS030526502 | GSK256066 (2,2,2-trifluoroacetic acid) | HY-70069 | MS-30869 | Trifluoroacetic acid--6-[3-(dimethylcarbamoyl)benzene-1-sulfonyl]-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide (1/1) | 1415560-64-3 | F84904 | GSK256066 (Trifluoroaceta
CAS number1415560-64-3molecular formulaC29H27F3N4O7S
molecular weight632.61 g/molExact mass≥99%
PSA177.000 Ųlogp-

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