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GSK256066(2,2,2-trifluoroaceticacid)

产品详情:

更新时间: 2025-09-06 14:22:50

CAS号:1415560-64-3

常用名: GSK 256066三氟乙酸盐

价格:

纯度: 98.0%

备货期: 10天

库存: 现货

其他详情(用途,包装):
用途: GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.IC50 value: 3.2 pM [1]Target: PDE4Bin vitro: GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity [1].in vivo: GSK256066 inhibits the LPS-induced pulmonary neutrophilia with an ED50 of 1.1 μg/kg, achieving maximal inhibition of 72% at 30 μg/kg when given in the aqueous suspension. GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 μg/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat [1]. GSK256066 sustains at a high lung concentration of 2.6 μg/g after intra-tracheal administration as an aqueous suspension at a dose of 30 μg/kg in rats [2]. GSK256066 (10 μg/kg) is administered intratracheally at different times (2, 6, 12, 18, 24, and 36 hours) before LPS administration, inhibiting LPS-Induced Pulmonary Neutrophilia in rat lipopolysaccharide (LPS)-induced models of acute pulmonary inflammation. GSK256066 (0.3–100 μg/kg) inhibits LPS-induced increases in exhaled nitric oxide with ED50 of 35 μg/kg in rat. GSK256066 (10 μg/kg) is administered half a hour before OVA administration in rat, inhibiting OVA-induced pulmonary eosinophilia with ED50 of 0.4 μg/kg. GSK256066 administered intratracheally as a dry powder blended in respiratory-grade lactose at doses of 3 to 100 μg/kg 2 hours before inhaled LPS challenge in ferrets, inhibiting LPS-induced pulmonary neutrophilia with ED50 of 18 μg/kg without inducing emetic episodes [3]. 物理化学性质: CAS号:1415560-64-3 常用中文名:GSK 256066三氟乙酸盐 常用英文名:GSK256066 (2,2,2-trifluoroacetic acid) 分子式:C29H27F3N4O7S 分子量:632.60700 密度:N/A 沸点:N/A 熔点:N/A 闪点:N/A 储存条件:2-8℃

供应商信息:

公司名:上海化源生化科技有限公司 推荐

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区域:上海市普陀区

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联系人:化源

产品详情: GSK256066(2,2,2-trifluoroaceticacid)


公司名:上海阿拉丁生化科技股份有限公司

区域:上海市浦东新区

价格:
¥6696.9/50mg ¥2325.9/10mg ¥1300.9/5mg

联系人:阿拉丁

产品详情: GSK256066 Trifluoroacetate


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2025-02-05 价格:¥6696.9 GSK256066 Trifluoroacetate

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GSK 256066三氟乙酸盐价格

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GSK256066(2,2,2-trifluoroaceticacid)价格为, 由GSK256066(2,2,2-trifluoroaceticacid)生产厂家上海化源生化科技有限公司提供,供应信息包括纯度,备货期/库存,供货能力等。>>电脑版:GSK256066(2,2,2-trifluoroaceticacid)_价格_生产厂家【上海化源生化科技有限公司】

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