Verteporfin

For research use only. Not for use in humans.

目录号:S1786 别名: CL 318952, Visudyne

Verteporfin  Chemical Structure

CAS No. 129497-78-5

Verteporfin (CL 318952, Visudyne) 是一种能够抑制YAP-TEAD相互作用的小分子化合物,抑制YAP诱导的肝脏过度生长。同时,它还是一种有效的衍生自卟啉的第二代光敏剂。Verteporfin 是一种自噬抑制剂。Verteporfin 可抑制细胞增殖并诱导凋亡。

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产品安全说明书

VDA抑制剂选择性比较

生物活性

产品描述 Verteporfin (CL 318952, Visudyne) 是一种能够抑制YAP-TEAD相互作用的小分子化合物,抑制YAP诱导的肝脏过度生长。同时,它还是一种有效的衍生自卟啉的第二代光敏剂。Verteporfin 是一种自噬抑制剂。Verteporfin 可抑制细胞增殖并诱导凋亡。
靶点
VDA [1]
(Endothelial cells)
YAP/TEAD interaction [3]
体外研究

对于穿透组织最好的波长(i.e.,大约700 nm)下的吸收光,Verteporfin比hematoporphyrin大约有效4倍,从而比hematoporphyrin提供了更高的细胞毒性(在人贴壁细胞中10倍以上)。Verteporfin是亲脂性的,与正常细胞或静息细胞相比,更容易被恶性的或激活的细胞摄取。Verteporfin与LDL结合形成一个复合物,随后可能通过LDL受体或者內吞作用被增殖细胞 (例如,新生血管内皮细胞) 摄取。Verteporfin疗法通过血管通道中形成血栓实现新生血管区的血管造影完全闭塞,进而引起选择性血管内皮损伤。Verteporfin疗法选择性诱导可再生的和离体的脉络膜毛细血管闭塞,而不改变覆盖的光感受器或神经节细胞,如光学和电子显微镜所示。[1] HL-60细胞中胱天蛋白酶-3和胱天蛋白酶-9的活化以及PARP的裂解映射出,光存在下,Verteporfin快速使细胞凋亡改变,该改变会被普通半胱天冬酶抑制剂ZVAD.fmk阻断。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL-60 MX;GeY5kfGmxbjDhd5NigQ>? NWj1bWV6hjFyMDDu[{9uVA>? MoDSSG1UVw>? M4HNV4lv[3KnYYPld{BFVkFiZoLh[41mdnSjdHnvckBt\X[nbIO= MX6xNFYxPzdzMB?=
HL-60 MXjjfZRwfG:6aXPpeJkh[XO|YYm= NU\BcVM6hjFyMDDu[{9uVA>? NWfI[G1ITE2VTx?= MY\pcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? NWfNT3NwOTB4MEe3NVA>
Jurkat MUHBdI9xfG:|aYOgZZN{[Xl? M2HlcZ4zQDBibl2= NIXxNohFVVOR NWjF[4c5cW6mdXPld{BiKEKlbD2yMYRmeGWwZHXueEBieG:ydH;zbZM> NWPncYJ[OTF{NEW0NVU>
RIF-1 M1z0T2Z2dmO2aX;uJIF{e2G7 MkDPNUDPxGdxbXy= NGXmb4FFVVOR NU\Q[mRt\GWlcnXhd4V{KG:6eXflckBkd26|dX3weIlwdg>? NF3HW3UyOjZzNUexPC=>
RIF-1 MUXjfZRwfG:6aXPpeJkh[XO|YYm= NUjZUpZbOSEQvHevcYw> NVXqO2RyTE2VTx?= MnTL[IVkemWjc3WgeI8hOjBiwsGgOUUh[2WubDDzeZJ3cX[jbB?= MnjKNVI3OTV5MUi=
SVEC4-10 NFz6NIhHfW6ldHnvckBie3OjeR?= M2TXeVIxOCCwZz;tcC=> MnnjSG1UVw>? M2XtVYlv\HWlZYOgcYlkem:2dXL1cIUh\GWyb3z5cYVzcXqjdHnvci=> M4j4[VE3PDZ5MUC2
SVEC4-10 MUDGeY5kfGmxbjDhd5NigQ>? NEXQOIczODBibnevcYw> NH[2XHZFVVOR NF;rOpRqdmS3Y3XzJJN1emW|czDhZ5RqdiCoaXLldkBnd3KvYYTpc44> MWCxOlQ3PzFyNh?=
ARPE-19 NVLa[2N3[3m2b4TvfIlkcXS7IHHzd4F6 M2PIdJ4xNjFizsznM41t NFvRXppFVVOR MUfzbI94eyCjIHTvd4Uu\GWyZX7k[Y51KHSxeHnjbZR6 MUexOlk5PzlyNR?=
ARPE-19 M3LsZmZ2dmO2aX;uJIF{e2G7 MX6wMlAyKM7:Zz;tcC=> NGi4VVdFVVOR MnT0bY5kemWjc3XzJHZGT0ZiYX7kJJJm\HWlZYOgVGVFTiCneIDy[ZN{cW:w NUfETG1SOTZ7OEe5NFU>
Y-79 NHnKVVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWXBfJRwhjFizsznM41t M2ThbmROW09? NX3ZR3FI\GWlcnXhd4V{KHKndHnuc4Jt[XO2b33hJINmdGxicILvcIln\XKjdHnvci=> MYixPFU4QTd4NB?=
WERI-Rb1 NVK5UZRtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkX1glEh|rypL33s MUTEUXNQ NWT2XG41\GWlcnXhd4V{KHKndHnuc4Jt[XO2b33hJINmdGxicILvcIln\XKjdHnvci=> MV2xPFU4QTd4NB?=
RB247C3 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVfjfmVihjFizsznM41t NWDz[ndITE2VTx?= NUjUcG0x\GWlcnXhd4V{KHKndHnuc4Jt[XO2b33hJINmdGxicILvcIln\XKjdHnvci=> MUixPFU4QTd4NB?=
RB355 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4nWXJ4yKM7:Zz;tcC=> NIrKOmNFVVOR NHfCS4xl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u MWSxPFU4QTd4NB?=
RB383 M1rPbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUe1dVFjhjFizsznM41t M2HVSWROW09? NXG1O|dV\GWlcnXhd4V{KHKndHnuc4Jt[XO2b33hJINmdGxicILvcIln\XKjdHnvci=> NGC1e24yQDV5OUe2OC=>
hFibro M2\uRYN6fG:2b4jpZ4l1gSCjc4PhfS=> NF7VVGcxNjViwsXnM41t M2PYfGROW09? MVjk[YNz\WG|ZYOgeoli[mmuaYT5JIJ6KDh4LEWl MWSyN|Q1OTFzNB?=
pTMC MYTjfZRwfG:6aXPpeJkh[XO|YYm= NVyzdpY5OC53INM1[{9udA>? MWDEUXNQ MVPk[YNz\WG|ZYOgeoli[mmuaYT5JIJ6KDl{Lkml NGDoXI4zOzR2MUGxOC=>
hTMC M2njWYN6fG:2b4jpZ4l1gSCjc4PhfS=> MYmwMlUhyrWpL33s MmPDSG1UVw>? NHSxS3Bl\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEi4Mlkm MX:yN|Q1OTFzNB?=
ARPE-19 NXvzPWZv[3m2b4TvfIlkcXS7IHHzd4F6 NEHJNVMxNjViwsXnM41t NXjl[G5WTE2VTx?= MXfk[YNz\WG|ZYOgeoli[mmuaYT5JIJ6KDV3LkWl Ml\JNlM1PDFzMUS=
Panc-1 MkTNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX[xNEDPxE1? MVzEUXNQ M{mxfolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NXPyU4gyOjRyNkmwOlk>
MIA PaCa-2 MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV[xNEDPxE1? NWHvN4k3TE2VTx?= NHHLN2dqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> Ml7sNlQxPjlyNkm=
BxPC-3 M37hWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFLHdWgyOCEQvF2= NFjpZZFFVVOR MVfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZ49ueGyndHXsfS=> NETYNZMzPDB4OUC2PS=>
SU86.86 NHnWXlNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXyxNEDPxE1? NG\lXnBFVVOR Mnv6bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJINwdXCuZYTlcJk> MXSyOFA3QTB4OR?=
MCF-7 MUnBeZRweGijZ4mgZZN{[Xl? Mmq1NVAh|ryP M4DWRWROW09? MoHubY5pcWKrdIOg[4Vu[2m2YXLpcoUucW6mdXPl[EBifXSxcHjh[5k> MYmyOFA3QTB4OR?=
WERI MkPRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYT+NVAh|rypL33s NYn2clJOTE2VTx?= NWWy[2lVcW6qaXLpeJMh\3Kxd4ToJI9nKHKndHnuc4Jt[XO2b33hJINmdGy| MVeyOFg{PzF2Mh?=
WERI M1:yeWZ2dmO2aX;uJIF{e2G7 MV7+NVAh|rypL33s MWLEUXNQ MljXZoxw[2u|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> NVLIUGhtOjR6M{exOFI>
Y-79 MmfOSpVv[3Srb36gZZN{[Xl? NIrJdIR,OTBizsznM41t MYjEUXNQ MnTwZoxw[2u|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44> MUOyOFg{PzF2Mh?=
Y-79 NFr2Z5hHfW6ldHnvckBie3OjeR?= M1\ucZ4yOCEQvHevcYw> NYfpd411TE2VTx?= MXfh[oZm[3S|IGnBVE1VTUGGIIDyc5RwNW:wY3;n[Y5mKHCjdHj3ZZk> NHLNXIkzPDh|N{G0Ni=>
Y-79 NFG3XmhHfW6ldHnvckBie3OjeR?= M1jF[54yOCEQvHevcYw> NF34NZpFVVOR MnnJ[I94di2{ZXf1cIF1\XNicHz1dolxd3SnbnP5JI1iemuncjDPR3QuPA>? NFzyeYQzPDh|N{G0Ni=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-S6(S240/244) / p-4EBP1(S65); 

PubMed: 28202507     


KLE, EFE184 and NOU-1 were treated with Verteporfin (0.1 μM, 0.3 μM). After 36h, cell lysates were western blotted with indicated antibodies. Bands are from one of three independent experiments.

c-Myc / Bcl-2; 

PubMed: 29416644     


In CAL27 cell lines, the expression of BCL-2 and C-MYC proteins decreased with the increase of Verteporfin concentration. The presented columns are given as the means ± SD. *p < 0.05, **P < 0.01, ***p < 0.001.

ECAD / Vimentin / Sox2 / CD44 / CD133; 

PubMed: 30467925     


Yes-associated protein 1 (YAP1), E-cadherin, vimentin (epithelial-mesenchymal transition [EMT] pathway), SOX2 CD44 and CD133 (autophagy markers) were detected by western blot in control, verteporfin (1 μmol/L) and verteporfin + 231-taxol (0.5 μmol/L) resistance groups.

beta-catenin; 

PubMed: 28202507     


KLE, EFE184, NOU-1 and SKUT-2 were treated with 3 μM Verteporfin. After 24h, cell lysates were western blotted with indicated antibodies. Bands are from one of three independent experiments.

28202507 29416644 30467925
Growth inhibition assay
Cell viability; 

PubMed: 28042502     


A: Cell viability was determined by MTS assay after the UM cells were exposed to verteporfin for 72 hours. B: After treated with various concentrations of verteporfin for 24 hours, the UM cells (e.g., 92.1, Mel 270, Omm 1, Omm 2.3) were seeded in drug-free soft agar culture for 14 days. Colonies were counted. 

28042502
Immunofluorescence
YAP1; 

PubMed: 30254296     


Treatment of U343 cells with 5 μM VP between 1-8 h in both 21% and 1% O2 induced morphological changes. Scale bar represents 10 µm. VP: Verteporfin

Calreticulin; 

PubMed: 30254296     


Calreticulin (CRT) significantly increased in VP-treated (5 µM, 2 h) U87 cells in both 21% and 1% O2 indicating likely ER stress.

p-YAP(Y357); 

PubMed: 28404908     


Confocal images of HEC-1-B cells and organoids which were subjected to immunofluorescence detection of A. YAP and B. phospho-YAP after VP treatment. YAP and phospho-YAP are conjugated with goat anti-mouse and goat anti-rabbit Alexa flour secondary antibodies respectively. (A) Upper panel bar=63x and lower panel bar = 20x. (B) Upper panel bar=63x and lower panel bar = 20x.

30254296 28404908
体内研究 Verteporfin可用于脉络膜血管和CNV的血管可视化,这表明光敏剂在猴子的实验性CNV中快速集聚。Verteporfin在建立的兔子眼睛的脉络膜脉管系统,RPE,以及光感受器中迅速积累。在小鼠体内,静脉注射3小时后,Verteporfin达到最大组织水平,随后在24小时内迅速下降。Verteporfin在体内代谢为活性较低的形式,并且迅速清除,主要通过粪便排泄,一小部分通过尿液排泄。Verteporfin疗法有效的选择性阻止了荧光染料从实验性诱导的猴子CNV的泄漏。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 100 mg/mL (139.12 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 718.79
化学式

C41H42N4O8

CAS号 129497-78-5
储存条件 粉状
溶于溶剂
别名 CL 318952, Visudyne

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03797547 Active not recruiting Other: AFLIBERCEPT Myopic Choroidal Neovascularisation Poitiers University Hospital June 22 2018 --
NCT01846273 Completed Drug: Ranibizumab|Drug: Verteporfin PDT|Drug: Sham PDT Age-related Macular Degeneration|Polypoidal Choroidal Vasculopathy Novartis Pharmaceuticals|Novartis August 7 2013 Phase 4
NCT00423189 Terminated Drug: Ranibizumab (Lucentis)|Drug: 0.5mg ranibizumab Age-Related Macular Degeneration David M. Brown M.D.|Novartis Pharmaceuticals|Greater Houston Retina Research January 2007 Phase 4
NCT00403442 Terminated Device: Verteporfin Therapy/ Drug: Bevacizumab Macular Degeneration Vitreous -Retina- Macula Consultants of New York|QLT Inc. September 2006 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID