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CI-1044  ≥98%

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包装规格：5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(100mg/ml 超声)
产品描述：基本信息 产品编号： C11279 产品名称： CI-1044 CAS: 197894-84-1   储存条件 粉末 -20℃ 四年     分子式： C23H19N5O2 溶于液体 -80℃ 六个月 分子量 397.43 -20℃ 一个月 化学名：  (R)-N-(9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-3-yl)nicotinamide Solubility (25°C)：   体外:   DMSO 125mg/mL(314.52mM;Need ultrasonic) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline，Solubility:≥2.08mg/mL(5.23mM);Clear solution 此⽅案可获得≥2.08mg/mL(5.23mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.08mg/mL(5.23mM);Clear solution 此⽅案可获得≥2.08mg/mL(5.23mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.5162mL 12.5808mL 25.1617mL 5mM 0.5032mL 2.5162mL 5.0323mL 10mM 0.2516mL 1.2581mL 2.5162mL   生物活性 产品描述 一种口服有效的 PDE4 抑制剂。 靶点 PDE4A5 0.29μM(IC50) PDE4B2 0.08μM(IC50) PDE4C2 0.56μM(IC50) PDE4D3 0.09μM(IC50) 体外研究 CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively. CI-1044 selectively inhibits PDE4 crude extract from U937 cells with an IC50 value of 0.27±0.02μM being threefold more potent than rolipram (IC50=0.91±0.14) and tenfold less potent than cilomilast (IC50=0.026±0.007) in the same assay. In the presence of PDE4 inhibitors, the production of TNF-α is dose dependently decreased with mean IC50 values from three separate experiments of 0.31±0.05, 0.26±0.05 and 0.11±0.01μM, for CI-1044, cilomilast and rolipram, respectively 体内研究 TNF-α production is dose-dependently inhibited by CI-1044, rolipram and cilomilast with ID50s of 0.4, 1.4 and 1.6 mg/kg respectively following single oral administration. Following repeated administration with CI-1044, the ID50 value represents 0.5 mg/kg p.o.. CI-1044 plasma levels increase proportionally with doses ranging between 0.1 and 40 mg/kg p.o. (R2=0.878). CI-1044 dose dependently inhibits the accumulation of eosinophils in Bronchoalveolar lavages (BAL) fluids with an ID50 value of 3.25 mg/kg. A single dose treatment with CI-1044 (10 mg/kg, p.o.) 24, 8, 3 or 1 h before the antigen challenge induces 6, 56, 48 and 79% inhibition in the number of eosinophils in BAL   推荐实验方法(仅供参考) Cell Assay Blood from anesthetized rats is collected in heparin tubes, immediately distributed in 96-well microplates (250μL/well) and incubated for 30 min at 37°C/5% CO2. Twenty-five microliters of vehicle or increasing concentrations of CI-1044, rolipram, cilomilast or solvant (saline/DMSO<0.1%) are added in wells and incubated for 30 min before the addition of LPS (100 μ g/mL) or saline. Plasma is removed after a 22 to 24 h incubation at 37°C/5% CO2, transferred in another 96-well microplate and stored at ) -80°C until a TNF-α assay by ELISA Animal Administration Male rats (200 to 220 g) are used and receive either vehicle or CI-1044 orally at 0.4, 1, 4, 10 and 40 mg/kg. In the single administration experiment, all treatments are given 1 h before blood collection. In the repeated administration experiment, the treatments are given twice a day during 13 days and once on day 14, 1 h before blood sampling
保存条件：-20℃

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