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GSK256066 (2,2,2-trifluoroacetic acid)

    
≥98%

GSK256066 (2,2,2-trifluoroacetic acid)

源葉(MedMol)
S83185 一鍵復制產品信息
1415560-64-3
C29H27F3N4O7S
632.6075
貨號 規格 價格 上海 北京 武漢 南京 購買數量
S83185-5mg
≥98% ¥1200.00 貨期:2-3天 - - -
S83185-10mg
≥98% ¥2200.00 貨期:2-3天 - - -
S83185-50mg
≥98% ¥6400.00 貨期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease

產品描述: GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease
靶點: IC50: 3.2 pM (PDE4B);PDE
體外研究: 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 IC50 of 0.01 nM
體內研究: 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. 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.
參考文獻: 1. Tralau-Stewart CJ, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration 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.
溶解性: soluble  in  DMSO
保存條件: -20℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 1.581 ml 7.904 ml 15.808 ml
5 mM 0.316 ml 1.581 ml 3.162 ml
10 mM 0.158 ml 0.79 ml 1.581 ml
50 mM 0.032 ml 0.158 ml 0.316 ml
注意: 部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。

參考文獻

質檢證書(COA)

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請輸入貨號和一個與之匹配的批號。
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批號:JS298415 貨號:S20001-25g
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摩爾濃度計算器

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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