Verteporfin

目录号:S1786 别名: CL 318952

Verteporfin  Chemical Structure

Molecular Weight(MW): 718.79

Verteporfin 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。

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客户使用该产品的3个实验数据:

  • Verteporfin treatment inhibits proliferation and induces apoptosis of Tsc1-null cells in vivo. Mice were administered i.p. with vehicle or verteporfin at a dose of 100 mg/kg every other day for 10 d before sacrifice. Mice were sacrificed at 6 wk of age. Three independent experiments were performed and mice in different treatments were pooled for analysis. Percentage of Ki67 and αSMA double-positive cells in α-SMA+ mesenchymal lesions in the indicated kidneys. Immunofluorescence staining and counting were performed on three sagittal sections from different kidney regions for each mouse.

    J Exp Med 2014 211(11), 2249-63. Verteporfin purchased from Selleck.

    The indicated cell lines were treated with control (Ctrl) or YAP-targeting siRNAs and growth assessed by XTT proliferation assays at the indicated time points. The mean and +SD are shown for three independent experiments. (Left panel, *, P < 0.05, significantly different from U87Rictor DMSO; Right panel, *, P < 0.05, significantly different from H4Rictor DMSO).

    J Biol Chem, 2015, 290(32): 19387-401 . Verteporfin purchased from Selleck.

  • The levels of YAP, phospho-YAP (S127), and its downstream targeted molecules CTGF and CYR61 were analyzed by Western blotting after UM cells were exposed to verteporfin for 24 hours.

    Am J Cancer Res, 2016, 6(12):2816-2830.. Verteporfin purchased from Selleck.

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 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。
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 MWnGeY5kfGmxbjDhd5NigQ>? NYjSN|VnhjFyMDDu[{9uVA>? NVPXPFh6TE2VTx?= NYjsfJBDcW6lcnXhd4V{KESQQTDmdoFodWWwdHH0bY9vKGyndnXsdy=> NUnwZXp{OTB4MEe3NVA>
HL-60 NIXCNFRkgXSxdH;4bYNqfHliYYPzZZk> M1jteJ4yODBibnevcWw> NWjCOI9KTE2VTx?= NWrETFZTcW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= MlzvNVA3ODd5MUC=
Jurkat NH;qO4RCeG:ydH;zbZMh[XO|YYm= M1XTc54zQDBibl2= NGqxdZNFVVOR NGfX[HhqdmS3Y3XzJIEhSmOuLUKt[IVx\W6mZX70JIFxd3C2b4Ppdy=> NVv2bW1OOTF{NEW0NVU>
RIF-1 Mn3BSpVv[3Srb36gZZN{[Xl? MoTjNUDPxGdxbXy= M1LWbWROW09? MVXk[YNz\WG|ZYOgc5h6\2WwIHPvcpN2dXC2aX;u M2rwSFEzPjF3N{G4
RIF-1 M1P2VoN6fG:2b4jpZ4l1gSCjc4PhfS=> NV62WY5EOSEQvHevcYw> M4T0RmROW09? NHzFPXZl\WO{ZXHz[UB1dyB{MDFCtUA2LSClZXzsJJN2en[rdnHs NGPCVYUyOjZzNUexPC=>
SVEC4-10 MYHGeY5kfGmxbjDhd5NigQ>? NILhWm0zODBibnevcYw> NVLmbmF2TE2VTx?= Moj1bY5lfWOnczDtbYNzd3S3YoXs[UBl\XCxbInt[ZJqgmG2aX;u NXnQ[G56OTZ2NkexNFY>
SVEC4-10 NEC2dmtHfW6ldHnvckBie3OjeR?= MWOyNFAhdmdxbXy= Mn:3SG1UVw>? NXT3NWlqcW6mdXPld{B{fHKnc4OgZYN1cW5iZnni[ZIh\m:{bXH0bY9v M1\Lc|E3PDZ5MUC2
ARPE-19 M3PUWoN6fG:2b4jpZ4l1gSCjc4PhfS=> NH[wXmd,OC5zIN88[{9udA>? NFfZXm5FVVOR NGXZNHZ{cG:5czDhJIRwe2VvZHXw[Y5l\W62IITvfIlkcXS7 MoP4NVY6QDd7MEW=
ARPE-19 MULGeY5kfGmxbjDhd5NigQ>? MV:wMlAyKM7:Zz;tcC=> NVnGPIZXTE2VTx?= NETrNYtqdmO{ZXHz[ZMhXkWJRjDhcoQhemWmdXPld{BRTUSIIHX4dJJme3Orb36= MYCxOlk5PzlyNR?=
Y-79 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MofBglEh|rypL33s MkXESG1UVw>? NXTNXYJD\GWlcnXhd4V{KHKndHnuc4Jt[XO2b33hJINmdGxicILvcIln\XKjdHnvci=> MkP6NVg2Pzl5NkS=
WERI-Rb1 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NES3ZVh,OSEQvHevcYw> MmjWSG1UVw>? MlXn[IVkemWjc3XzJJJmfGmwb3LsZZN1d22jIHPlcIwheHKxbHnm[ZJifGmxbh?= M3uwWFE5PTd7N{[0
RB247C3 NIroZo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFr6XWt,OSEQvHevcYw> MV7EUXNQ MmPi[IVkemWjc3XzJJJmfGmwb3LsZZN1d22jIHPlcIwheHKxbHnm[ZJifGmxbh?= NY\vXHNrOTh3N{m3OlQ>
RB355 MnjBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYrRcGp6hjFizsznM41t M3qzZWROW09? MYfk[YNz\WG|ZYOgdoV1cW6xYnzhd5RwdWFiY3XscEBxem:uaX\ldoF1cW:w NVzWPHlxOTh3N{m3OlQ>
RB383 M3uxfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4HYRZ4yKM7:Zz;tcC=> MVPEUXNQ MWDk[YNz\WG|ZYOgdoV1cW6xYnzhd5RwdWFiY3XscEBxem:uaX\ldoF1cW:w MlXGNVg2Pzl5NkS=
hFibro MmT2Z5l1d3SxeHnjbZR6KGG|c3H5 NELPTlcxNjViwsXnM41t MYPEUXNQ NIX3PGpl\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEi2MFUm MV2yN|Q1OTFzNB?=
pTMC MVLjfZRwfG:6aXPpeJkh[XO|YYm= MmLDNE42KML3Zz;tcC=> MXTEUXNQ M2fGWIRm[3KnYYPld{B3cWGkaXzpeJkh[nliOUKuPUU> M4eyOVI{PDRzMUG0
hTMC M2jxXYN6fG:2b4jpZ4l1gSCjc4PhfS=> MmPXNE42KML3Zz;tcC=> NXHQXpFXTE2VTx?= NELSWm9l\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEi4Mlkm MkmwNlM1PDFzMUS=
ARPE-19 MVzjfZRwfG:6aXPpeJkh[XO|YYm= NI\xW4YxNjViwsXnM41t MXrEUXNQ NIPnPFll\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEW1MlUm M{jSVVI{PDRzMUG0
Panc-1 M2DZ[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3XpdVExKM7:TR?= NU[5WmRtTE2VTx?= MnfabY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MlXYNlQxPjlyNkm=
MIA PaCa-2 MnrUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4nSNlExKM7:TR?= MkjxSG1UVw>? NHvidohqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MkH4NlQxPjlyNkm=
BxPC-3 M3zp[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{[2UVExKM7:TR?= MnywSG1UVw>? MlnBbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJINwdXCuZYTlcJk> MoXjNlQxPjlyNkm=
SU86.86 NHraclBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHTCbZIyOCEQvF2= Mnz1SG1UVw>? NEDwfo9qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[2:vcHzleIVtgQ>? MXmyOFA3QTB4OR?=
MCF-7 NH2xOnlCfXSxcHjh[5kh[XO|YYm= NXLtfpozOTBizszN M{Xp[mROW09? NWHPelFOcW6qaXLpeJMh\2WvY3n0ZYJqdmVvaX7keYNm\CCjdYTvdIhi\3l? M1vWSVI1ODZ7ME[5
WERI M4PscWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGPlW|R,OTBizsznM41t M1HkVWROW09? MWrpcohq[mm2czDndo94fGhib3[gdoV1cW6xYnzhd5RwdWFiY3XscJM> MXyyOFg{PzF2Mh?=
WERI MVvGeY5kfGmxbjDhd5NigQ>? Ml;kglExKM7:Zz;tcC=> M4HuOmROW09? MXvicI9kc3NiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> MYOyOFg{PzF2Mh?=
Y-79 MmriSpVv[3Srb36gZZN{[Xl? NHz2[5Z,OTBizsznM41t NXnjZlVbTE2VTx?= NEfxPGJjdG:la4OgZ4VtdCCleXPs[UBxem:pcnXzd4lwdg>? MoO1NlQ5OzdzNEK=
Y-79 MVHGeY5kfGmxbjDhd5NigQ>? NY\0XXpohjFyIN88[{9udA>? MoO4SG1UVw>? NV2xN2Zu[W[oZXP0d{B[SVBvVFXBSEBxem:2bz3vcoNw\2WwZTDwZZRpf2G7 MoTxNlQ5OzdzNEK=
Y-79 MUXGeY5kfGmxbjDhd5NigQ>? MU\+NVAh|rypL33s NEnWPJdFVVOR MXvkc5dvNXKnZ4XsZZRmeyCybIXybZBwfGWwY4mgcYFzc2W{IF;DWE01 M4LFZ|I1QDN5MUSy

... Click to View More Cell Line Experimental Data

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
稳定性 powder
in solvent
别名 CL 318952

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT01846273 Completed Age-related Macular Degeneration|Polypoidal Choroidal Vasculopathy PCV Novartis Pharmaceuticals|Novartis August 7 2013 Phase 4
NCT02939274 Recruiting Metastatic Breast Cancer Rogers Sciences Inc. October 2016 Phase 2
NCT01968486 Completed Myopia Degenerative University of Campania Luigi Vanvitelli June 2012 Phase 1
NCT00674323 Completed Polypoidal Choroidal Vasculopathy Novartis April 2008 Phase 4
NCT00574093 Completed Neovascular Age Related Macular Degeneration Fondazione G.B. Bietti IRCCS January 2008 Phase 2
NCT00433017 Terminated Macular Degeneration|Choroidal Neovascularization Novartis May 2007 Phase 2|Phase 3

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操作手册

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VDA Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID