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EG00229  ≥98%

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包装规格：5mg in glass bottle
溶解性：溶于DMSO（≥41.4mg/mL）
产品描述：基本信息 产品编号： E10438 产品名称： EG00229 CAS: 1210945-69-9   储存条件 粉末 -20℃ 四年     分子式： C19H20F3N7O7S3 溶于液体 -80℃ 六个月 分子量 611.60 -20℃ 一个月 化学名：  (2S)-2-[[3-(2,1,3-benzothiadiazol-4-ylsulfonylamino)thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid;2,2,2-trifluoroacetic acid Solubility (25°C)：   体外:   DMSO ≥41.4mg/mL(67.69mM) 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(4.09mM);Clear solution 此⽅案可获得≥2.5mg/mL(4.09mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-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% corn oil Solubility:≥2.5mg/mL(4.09mM);Clear solution 此⽅案可获得≥2.5mg/mL(4.09mM，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100μL25.0mg/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 1.6351mL 8.1753mL 16.3506mL 5mM 0.3270mL 1.6351mL 3.2701mL 10mM 0.1635mL 0.8175mL 1.6351mL   生物活性 产品描述 一种神经纤维蛋白 1 受体 (NRP1) 拮抗剂。 靶点 IC50: 8μM (125I-VEGF-A binding to PAE/NRP1); 3μM (bt-VEGF-A binding to purified NRP1 b1 domain) 体外研究 EG00229 (Compound 2; 0-100μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation EG00229 (Compound 2) demonstrates inhibition of VEGF-A binding to NRP1 and attenuates VEGFR2 phosphorylation in endothelial cells. Inhibition of migration of endothelial cells is also observed in HUVECs EG00229 (Compound 2) selectively inhibits radiolabeled 125I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1, but not VEGFR2-expressing cells, with an IC50 of 8μM. EG00229 also inhibits VEGF-A binding to lung carcinoma A549 and prostate carcinoma DU145 cells, which express NRP1, but not VEGFR1 and VEGFR2, with similar potency. Binding of VEGF-A to human umbilical vein endothelial cells (HUVECs), which express VEGFR2, VEGFR1, and NRP1, is also inhibited by EG00229 with an IC 50 of 23μM Cell Viability Assay Cell Line: A549 cells Concentration: 0µM,10μM,30μM,100μM Incubation Time: 48 hours Result: Caused a significant reduction in cell viability. 体内研究 EG00229 (0-10 mg/kg; intraperitoneal injection; three times per week; for 4 weeks; NSG mice) treatment substantially reduces tumor growth and visible vascularization Animal Model: 6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells Dosage: 0mg/kg,10mg/kg Administration: Intraperitoneal injection; three times per week; for 4 weeks Result: Reduces tumor growth and visible vascularization.
保存条件：-20℃

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