NVP-BAW2881
產品名稱:NVP-BAW2881
產品描述:
產品描述 | 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. |
靶點活性 | hVEGFR2:9 nM, B-RAFV599E:76 nM, mVEGF2:165 nM, c-Abl:99 nM, C-Raf-1:24 nM |
體外活性 | 局部施用NVP-BAW2881在小鼠和家豬皮膚中,能減少VEGF-A誘導的血管通透性.NVP-BAW2881能夠靶向鼠源、豬源和人源VEGFR2的酪氨酸激酶區域.NVP-BAW2881減少小鼠的皮膚損傷處白細胞浸潤,減少表皮增生、正常表皮角化細胞分化以及顯示較少的血管異常.NVP-BAW2881處理過的小鼠的血管變小、數量減少.相較于對照組,實驗組小鼠的耳腫脹、皮膚炎癥、淋巴結腫大、皮膚紅斑得到改善.雖然兩種給藥途徑都有效(口服和局部施用),但全身性用藥比局部給藥更為強效. |
體內活性 | 體外實驗證明NVP-BAW2881能夠抑制人淋巴管內皮細胞和臍靜脈內皮細胞的增殖、遷移以及小管生成。 |
細胞實驗 | 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) |
別名 | BAW2881 |
分子量 | 424.383 |
分子式 | C22H15F3N4O2 |
CAS No. | 861875-60-7 |
存儲
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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公司介紹:
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發,涵蓋生物科技、化學品、中間體和化工材料等領域。
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