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Esonarimod  ≥98% (HPLC)

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包装规格：1mg 5mg in glass bottle
溶解性：溶于DMSO
产品描述：基本信息 产品编号： E10009 产品名称： Esonarimod CAS: 101973-77-7   储存条件 粉末 -20℃ 四年     分子式： C14H16O4S 溶于液体 -80℃ 两年 分子量 280.34 -20℃ 一个月 化学名：  2-Acetylthiomethyl-3-(4-methylbenzoyl)propionic acid Solubility (25°C)：   体外:   DMSO 100mg/mL (356.71mM; 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: ≥ 2.5mg/mL (8.92mM); Clear solution 此⽅案可获得 ≥ 2.5mg/mL (8.92mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0mg/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: ≥ 2.5mg/mL (8.92mM); Clear solution 此⽅案可获得 ≥ 2.5mg/mL (8.92mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 25.0mg/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: ≥ 2.5mg/mL (8.92mM); Clear solution 此⽅案可获得 ≥ 2.5mg/mL (8.92mM，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 25.0mg/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 3.5671mL 17.8355mL 35.6710mL 5mM 0.7134mL 3.5671mL 7.1342mL 10mM 0.3567mL 1.7835mL 3.5671mL   生物活性 产品描述 一种抗风湿化合物。 体外研究 Esonarimod (KE-298) (10 to 300μg/mL) suppresses the production of NO by RAW264.7 cells in a dose dependent manner. The IC50 of Esonarimod is 117.5μg/mL. Esonarimod does not affect cellular viability at these tested doses. Esonarimod has no direct effect on NOS activity in cell-free extracts of RAW264.7 cells 体内研究 After repeated oral administration of Esonarimod (14C-KE-298), the radioactivity decreases rapidly and no tendency towards accumulation is found   推荐实验方法(仅供参考) Kinase Assay Enzyme activity of NOS is determined using an assay kit for NOS activity. Briefly, the lysate from RAW264.7 cells (a protein concentration of 37.5μg/200μL) is incubated for 3 h at 37°C with 100mM of L-arginine in the presence of Esonarimod (KE298) and the conversion of L-arginine to nitrite is monitored. The nitrite generated in the reaction mixture is assayed using Griess reagent     Cell Assay RAW264.7 cells are used in this study. For NO production, RAW264.7 cells [2×105 /0.2mL of RPMI-1640 supplemented by 10% heat inactivated fetal bovine serum (FBS), penicillin G (100 U/mL), and streptomycin (100μg/mL)] are stimulated with 100ng/mL of Escherichia coli 026:B6 lipopolysaccharide in the presence of Esonarimod (KE-298) (0, 10, 30, 100, 200, 300μg/mL) in 96 well plates and incubated 24 h at 37°C in an atmosphere of 5% CO2 in air. After incubation, the supernatants are collected and assayed for nitrite (NO2-) instead of NO     Animal Administration Seven-week-old male Wistar rats are used in this study. The animals are fasted overnight before dosing and for up to 4 h after dosing, except for the study on tissue distribution after repeated oral administration. The rats are grouped, three or four rats per group. Esonarimod (14C-KE-298) is administered orally by gastric intubation in a dose of 5mg/kg once daily for 21 days. At 20 min, 24 h or 21 days after dosing with Esonarimod, the rats are anaesthetized with ether and blood samples are collected from the femoral aorta into heparinized containers. The liver, kidney, lung, aorta and skin are excised and weighed. Tissues (except aorta) are homogenized with ice-cold physiological saline to yield a 20% homogenate
保存条件：-20℃

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