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KN-93  ≥98% (HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO (25mg/ml)
产品描述：基本信息 产品编号： K10008 产品名称： KN-93 CAS: 139298-40-1   储存条件 粉末 -20℃ 四年     分子式： 139298-40-1 溶于液体 -80℃ 两年 分子量 599.03 -20℃ 1个月 化学名：  (E)-N-(2-(((3-(4-Chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide Solubility (25°C)：   体外:   DMSO 100 mg/mL (199.58mM) Ethanol 21 mg/mL (41.91mM) Water Insoluble 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: ≥ 0.83 mg/mL (1.66mM); Clear solution 此⽅案可获得 ≥ 0.83 mg/mL (1.66mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 8.3 mg/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: 0.83 mg/mL (1.66mM); Clear solution; Need ultrasonic and warming 此⽅案可获得 0.83 mg/mL (1.66mM) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility: ≥ 0.83 mg/mL (1.66mM); Clear solution 此⽅案可获得 ≥ 0.83 mg/mL (1.66mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例，取 100μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，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 1.9958mL 9.9792mL 19.9585mL 5mM 0.3992mL 1.9958mL 3.9917mL 10mM 0.1996mL 0.9979mL 1.9958mL 50mM 0.0399mL 0.1996mL 0.3992mL     生物活性 产品描述 一种具有磷酸化活性的CaMKII抑制剂，IC50：370nM。 靶点 Ki: 370nM (CaMK)   体外研究 After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, plateletderived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts. KN-93 inhibits the H+ , K+ -ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space. KN-93 (0.5μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca2+-independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93. KN-93 (10μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells. 体内研究 KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes, and suppresses phosphorylation of CaMKII and NF-κB in diabetic retina.   推荐实验方法(仅供参考) Cell Assay Cell viability is assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. Briefly, Müller cells are seeded at a density of 10×104 cells per well in 96-well plates and cultured until sub-confluence. Next, cells are treated with curcumin for 24 h before incubation with MTT (5 mg/mL) at 37°C in 5% CO2 atmosphere for 4 h. The culture medium is then removed, and the formazan formed in the reaction is dissolved in 150μL DMSO. The optical density of the solution is measured at 490nm using a multifunctional microplate reader. Cell viability in each well is presented as a percentage of the control (vehicle-treated group)   Animal Administration Male Sprague-Dawley rats (8 weeks of age) weighing 180-200 g are used in this study. Rats are housed in ventilated microisolator cages with free access to water and food. The rats are randomLy assigned to receive either 60 mg/kg STZ intraperitoneally or citrate buffer alone. Rats are categorized as diabetic when blood glucose levels exceeded 16.7mM at 48 h after STZ treatment. Two weeks after the induction of diabetes, rats are divided randomLy into three subgroups: STZdiabetic rats (n=12), STZ-treated diabetic rats administered curcumin (n=12), or STZ-diabetic rats administered KN93 (n=12) for a 12-week period. Curcumin is suspended in saline containing 0.5% carboxymethylcellulose at a concentration of 20 mg/mL and administered via oral gavage at a total dose of 100 mg/kg/day. KN93 is administered by intraperitoneal injection at 1 mg/kg/day. Control STZ-treated diabetic rats and non-diabetic controls (n=12) are gavage administered saline containing 0.5% carboxymethylcellulose on a daily basis. Body weights and blood glucose levels are measured every 2 weeks.
保存条件：-20℃

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