NVP-BAW2881
作者：齐岳
发布时间：2023-08-23
09:21:36
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产品名称：NVP-BAW2881
产品描述：
| 产品描述 | BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation. |
| 靶点活性 | hVEGFR2:9 nM, B-RAFV599E:76 nM, mVEGF2:165 nM, c-Abl:99 nM, C-Raf-1:24 nM |
| 体外活性 | 局部施用NVP-BAW2881在小鼠和家猪皮肤中,能减少VEGF-A诱导的血管通透性.NVP-BAW2881能够靶向鼠源、猪源和人源VEGFR2的酪氨酸激酶区域.NVP-BAW2881减少小鼠的皮肤损伤处白细胞浸润,减少表皮增生、正常表皮角化细胞分化以及显示较少的血管异常.NVP-BAW2881处理过的小鼠的血管变小、数量减少.相较于对照组,实验组小鼠的耳肿胀、皮肤炎症、淋巴结肿大、皮肤红斑得到改善.虽然两种给药途径都有效（口服和局部施用）,但全身性用药比局部给药更为强效. |
| 体内活性 | 体外实验证明NVP-BAW2881能够抑制人淋巴管内皮细胞和脐静脉内皮细胞的增殖、迁移以及小管生成。 |
| 细胞实验 | HUVECs or LECs (1.2×103) were seeded into fibronectin-coated 96-well plates. After 24 hours, the cells were transferred into LEC medium containing 2% fetal bovine serum and incubated for an additional 24 hours. Cells(eight wells/condition) were incubated with medium alone(control), 20 ng/ml VEGF-A, or a combination of 20 ng/ml VEGF-A and 1 nmol/L to 1 mol/L NVP-BAW2881. Proliferation was also assayed in LECs incubated with 500 ng/ml VEGF-C. The dimethyl sulfoxide concentration was adjusted to 0.1% in all wells. After 72 hours, cells were incubated with 5-methylumbelliferylheptanoate for subsequent fluorescent quantification of viable cells, using a SpectraMax Gemini electron microscope. (Only for Reference) |
| 别名 | BAW2881 |
| 分子量 | 424.383 |
| 分子式 | C22H15F3N4O2 |
| CAS No. | 861875-60-7 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 78 mg/mL (183.8 mM)
Ethanol: 16 mg/mL (37.7 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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