产品说明书
Verteporfin
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同义名 : | CL 318952;BPD-MA;DB00460, CL 318952, BPD-MA, BpdMA, Benzoporphyrin D, Benzoporphyrin derivative monoacid ring A, Verteporfin, Visudyne. |
| CAS号 : | 129497-78-5 | |
| 货号 : | A138297 | |
| 分子式 : | - | |
| 纯度 : | 98% | |
| 分子量 : | 0 | |
| MDL号 : | MFCD28098202 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO DMF: 10 mg/mL，配合低频超声，并水浴加热至45℃助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | Verteporfin (CL 318952) is utilized as a photosensitizer in photodynamic therapy aimed at eradicating abnormal blood vessels in the eye, particularly in conditions like age-related macular degeneration. It also functions as a YAP inhibitor, effectively disrupting YAP-TEAD interactions and inducing apoptosis in cells[1]. Additionally, Verteporfin acts as an autophagy inhibitor, specifically blocking the early stages of autophagy by preventing autophagosome formation[3]. | ||
| 作用机制 | Verteporfin is transported in the plasma primarily by lipoproteins and once been activated by light in the presence of oxygen, highly reactive, short-lived singlet oxygen and reactive oxygen radicals are generated. Light activation of verteporfin can locally damage neovascular endothelium, resulting in vessel occlusion. Damaged endothelium is known to release procoagulant and vasoactive factors through the lipo-oxygenase (leukotriene) and cyclo-oxygenase (eicosanoids such as thromboxane) pathways, resulting in platelet aggregation, fibrin clot formation and vasoconstriction. Verteporfin appears to somewhat preferentially accumulate in neovasculature, including choroidal neovasculature. However, animal models indicate that the drug is also present in the retina. As singlet oxygen and reactive oxygen radicals are cytotoxic, Verteporfin can also be used to destroy tumor cells. https://www.drugbank.ca/drugs/DB00460 | ||
| 细胞研究 | |||||
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| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| ARPE-19 | ~0.1 μg/ml | cytotoxicity assay | shows a dose-dependent toxicity | 16987905 | |
| ARPE-19 | 0.01 μg/ml | Function assay | increases VEGF and reduces PEDF expression | 16987905 | |
| ARPE-19 | 0.5 µg/ml | cytotoxicity assay | decreases viability by 55.5% | 23441114 | |
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00211484 | Age-Related Macular Degenerati... 展开 >>ons. Subfoveal Neovascularization. 收起 << | Phase 2 | Completed | - | United States, New York ... 展开 >> Manhattan Eye, Ear & Throat Hospital New York, New York, United States, 10021 收起 << |
| NCT02587767 | Acute Central Serous Chorioret... 展开 >>inopathy 收起 << | Not Applicable | Active, not recruiting | December 2018 | China, Guangdong ... 展开 >> Zhongshan Ophthalmic Center, Sun Yat-sen University Guangzhou, Guangdong, China, 510060 收起 << |
| NCT02072408 | Polypoidal Choroidal Vasculopa... 展开 >>thy Without Active Polyp 收起 << | Phase 4 | Completed | - | Korea, Republic of ... 展开 >> Seoul National University Bundang Hospital Seongnam, Gyunggi-do, Korea, Republic of Konyang University Kim's Eye Hospital Seoul, Korea, Republic of Samsung Medical Center Seoul, Korea, Republic of 收起 << |
| 参考文献 |
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