Verteporfin

製品コードS1786 バッチS178616

印刷

化学情報

Synonyms

CL 318952

Storage
(From the date of receipt)

3 years-20°C （in the dark）powder

化学式

C₄₁H₄₂N₄O₈

分子量

718.79

CAS No.

129497-78-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (139.12 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (6.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ベルテポルフィン (Verteporfin (CL 318952)) は、TEAD-YAP 相互作用と YAP による肝肥大を阻害します。また、ポルフィリンに由来する強力な第 2 世代の光増感剤でもあります。ベルテポルフィンはオートファジー (autophagy) 阻害剤です。ベルテポルフィンは細胞増殖を阻害し、アポトーシス (apoptosis) を誘導します。
in vitro	Verteporfin is about four times more efficient in absorbing light at wavelengths that penetrate tissues best (i.e., around 700 nm) and thus provides a much higher cytotoxic effect than hematoporphyrin (10 times more in human adherent cell lines). This compound is lipophilic and is more readily taken up by malignant or activated cells, compared with normal or resting cells. It binds with LDL to form a complex, which is then taken up into proliferating cells (e.g., neovascular endothelial cells) probably via LDL receptors and endocytosis. This therapy achieves complete angiographic occlusion of the neovascular compartment by thrombosis of vascular channels, following selective endothelial damage. It selectively induces reproducible and isolated choriocapillary occlusion without alteration of overlying photoreceptors or ganglion cells, as shown by light and electron microscopy. ^[1] This chemical conbined with light rapidly exhibits apoptotic changes reflected by caspase-3 and caspase-9 activation and PARP cleavage in HL-60 cells, changes that are blocked by the general caspase inhibitor ZVAD.fmk. ^[2]
in vivo	Verteporfin can be used for angiographic visualization of choroidal vessels and CNV, which demonstrates that the photosensitizer accumulates rapidly in experimental CNV in monkeys. This compound accumulates rapidly in the established vasculature of the choroid, RPE, and photoreceptors of rabbit eyes. It reaches maximal tissue levels within 3 hours of intravenous injection, followed by a rapid decline within 24 hours in mice. This chemical is metabolized to a less active form in vivo and is cleared very rapidly, predominantly in the feces and a very small proportion excreted in urine. The therapy effectively and selectively prevents fluorescein dye leakage from experimentally induced CNV in monkeys. ^[1]

製品説明

ベルテポルフィン (Verteporfin (CL 318952)) は、TEAD-YAP 相互作用 と YAP による肝肥大を阻害します。また、ポルフィリンに由来する強力な第 2 世代の光増感剤でもあります。ベルテポルフィンはオートファジー (autophagy) 阻害剤です。ベルテポルフィンは細胞増殖を阻害し、アポトーシス (apoptosis) を誘導します。

in vitro

Verteporfin is about four times more efficient in absorbing light at wavelengths that penetrate tissues best (i.e., around 700 nm) and thus provides a much higher cytotoxic effect than hematoporphyrin (10 times more in human adherent cell lines). This compound is lipophilic and is more readily taken up by malignant or activated cells, compared with normal or resting cells. It binds with LDL to form a complex, which is then taken up into proliferating cells (e.g., neovascular endothelial cells) probably via LDL receptors and endocytosis. This therapy achieves complete angiographic occlusion of the neovascular compartment by thrombosis of vascular channels, following selective endothelial damage. It selectively induces reproducible and isolated choriocapillary occlusion without alteration of overlying photoreceptors or ganglion cells, as shown by light and electron microscopy. ^[1]

This chemical conbined with light rapidly exhibits apoptotic changes reflected by caspase-3 and caspase-9 activation and PARP cleavage in HL-60 cells, changes that are blocked by the general caspase inhibitor ZVAD.fmk. ^[2]

in vivo

Verteporfin can be used for angiographic visualization of choroidal vessels and CNV, which demonstrates that the photosensitizer accumulates rapidly in experimental CNV in monkeys. This compound accumulates rapidly in the established vasculature of the choroid, RPE, and photoreceptors of rabbit eyes. It reaches maximal tissue levels within 3 hours of intravenous injection, followed by a rapid decline within 24 hours in mice. This chemical is metabolized to a less active form in vivo and is cleared very rapidly, predominantly in the feces and a very small proportion excreted in urine. The therapy effectively and selectively prevents fluorescein dye leakage from experimentally induced CNV in monkeys. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Ki67+ and Sox10+ cells
	濃度	2 uM
	反応時間	72 h
	実験の流れ	Cells were treated with verteporfin (2 µM) for 72 hr for Brdu staining.
動物実験	動物モデル	Atoh1-Ptch mice
	投薬量	100 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/11094244/
https://pubmed.ncbi.nlm.nih.gov/10607710/
https://pubmed.ncbi.nlm.nih.gov/22677547/

https://pubmed.ncbi.nlm.nih.gov/29438698/
https://pubmed.ncbi.nlm.nih.gov/31474569/

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by J Exp Med, 2014, 211(11), 2249-63]

: Data from [Data independently produced by , , Theranostics, 2017, 7(5):1114-1132]

: Data from [Data independently produced by , , Cancer Lett, 2018, 423:36-46]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Engineering anti-c-MET scFv-conjugated PLGA nanoparticles for precision verteporfin delivery in lung cancer cells: a formulation study [ Int J Pharm, 2025, 683:126004]	PubMed: 40730320

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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