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 MYPGeY5kfGmxbjDhd5NigQ>? MWL+NVAxKG6pL33M NWOwdlJSTE2VTx?= M{TNb4lv[3KnYYPld{BFVkFiZoLh[41mdnSjdHnvckBt\X[nbIO= MoD3NVA3ODd5MUC=
HL-60 MVHjfZRwfG:6aXPpeJkh[XO|YYm= NEHB[FF,OTByIH7nM41N NX21Ond{TE2VTx?= NVvGVm54cW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= NGL1ZoIyODZyN{exNC=>
Jurkat M2Pjc2Fxd3C2b4Ppd{Bie3OjeR?= MVj+NlgxKG6P M1TCR2ROW09? Mn\rbY5lfWOnczDhJGJkdC1{LXTldIVv\GWwdDDhdI9xfG:|aYO= NVnFTGhLOTF{NEW0NVU>
RIF-1 M1;Rc2Z2dmO2aX;uJIF{e2G7 MnqyNUDPxGdxbXy= MkLYSG1UVw>? Mnri[IVkemWjc3XzJI95gWenbjDjc45{fW2ydHnvci=> M4K1PFEzPjF3N{G4
RIF-1 NIX6[|dkgXSxdH;4bYNqfHliYYPzZZk> M4q2RlEh|rypL33s M{DZfmROW09? M1XmdoRm[3KnYYPlJJRwKDJyINMxJFUmKGOnbHygd5Vzfmm4YXy= M3HHeFEzPjF3N{G4
SVEC4-10 Mn;ZSpVv[3Srb36gZZN{[Xl? Ml;UNlAxKG6pL33s NInVOIFFVVOR M{X1V4lv\HWlZYOgcYlkem:2dXL1cIUh\GWyb3z5cYVzcXqjdHnvci=> MWGxOlQ3PzFyNh?=
SVEC4-10 NX64S|V1TnWwY4Tpc44h[XO|YYm= MWeyNFAhdmdxbXy= NHPjfFlFVVOR NWjpXVZXcW6mdXPld{B{fHKnc4OgZYN1cW5iZnni[ZIh\m:{bXH0bY9v MVexOlQ3PzFyNh?=
ARPE-19 M4HNToN6fG:2b4jpZ4l1gSCjc4PhfS=> MUH+NE4yKM7:Zz;tcC=> NGfxN5VFVVOR NV65Zms1e2ixd4OgZUBld3OnLXTldIVv\GWwdDD0c5hq[2m2eR?= MnXMNVY6QDd7MEW=
ARPE-19 NUDFTG42TnWwY4Tpc44h[XO|YYm= MWqwMlAyKM7:Zz;tcC=> MkTxSG1UVw>? MmLPbY5kemWjc3XzJHZGT0ZiYX7kJJJm\HWlZYOgVGVFTiCneIDy[ZN{cW:w MUixOlk5PzlyNR?=
Y-79 M2K5O2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTQR|Q1hjFizsznM41t NUi0WnliTE2VTx?= Mmfx[IVkemWjc3XzJJJmfGmwb3LsZZN1d22jIHPlcIwheHKxbHnm[ZJifGmxbh?= M2q2T|E5PTd7N{[0
WERI-Rb1 NVfCNIpKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zIep4yKM7:Zz;tcC=> M4e1NWROW09? NUTJPIhR\GWlcnXhd4V{KHKndHnuc4Jt[XO2b33hJINmdGxicILvcIln\XKjdHnvci=> NVrCNHN1OTh3N{m3OlQ>
RB247C3 MkHZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYTz[pc1hjFizsznM41t MkDFSG1UVw>? M4rYcYRm[3KnYYPld{Bz\XSrbn;icIF{fG:vYTDj[YxtKHC{b3zp[oVz[XSrb36= MnTJNVg2Pzl5NkS=
RB355 M3;mdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYH+NUDPxGdxbXy= MonmSG1UVw>? NIS1WpRl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u NFXLflEyQDV5OUe2OC=>
RB383 NYHVcJJPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoTDglEh|rypL33s NVr1[4pXTE2VTx?= M{izboRm[3KnYYPld{Bz\XSrbn;icIF{fG:vYTDj[YxtKHC{b3zp[oVz[XSrb36= NVTYO|ZqOTh3N{m3OlQ>
hFibro NIXqbIZkgXSxdH;4bYNqfHliYYPzZZk> MYmwMlUhyrWpL33s MoHaSG1UVw>? MV3k[YNz\WG|ZYOgeoli[mmuaYT5JIJ6KDh4LEWl M3\NRVI{PDRzMUG0
pTMC M1HacYN6fG:2b4jpZ4l1gSCjc4PhfS=> NHezNVkxNjViwsXnM41t M3zueWROW09? NHvIU5ll\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEmyMlkm MX2yN|Q1OTFzNB?=
hTMC M4Lxd4N6fG:2b4jpZ4l1gSCjc4PhfS=> M3nLVFAvPSEEtXevcYw> MoHsSG1UVw>? NV:2PHZU\GWlcnXhd4V{KH[rYXLpcIl1gSCkeTC4PE46LQ>? MX2yN|Q1OTFzNB?=
ARPE-19 NFe2fJNkgXSxdH;4bYNqfHliYYPzZZk> NGKzS5IxNjViwsXnM41t NHLLWmJFVVOR NHvTOIFl\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEW1MlUm NETydGUzOzR2MUGxOC=>
Panc-1 NVjYPG9lT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MY[xNEDPxE1? MUPEUXNQ NXK3Vo1LcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NVPzTWl1OjRyNkmwOlk>
MIA PaCa-2 Ml;ZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkfWNVAh|ryP MWnEUXNQ MWjpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NFnUO5MzPDB4OUC2PS=>
BxPC-3 NELhPHdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWXlOHFQOTBizszN MlXKSG1UVw>? MVTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZ49ueGyndHXsfS=> MlO4NlQxPjlyNkm=
SU86.86 M3\aZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV7qTXJuOTBizszN MX7EUXNQ NYTDSWwxcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGOxbYDs[ZRmdHl? MWmyOFA3QTB4OR?=
MCF-7 M2LLfGF2fG:yaHHnfUBie3OjeR?= MVexNEDPxE1? NVLXflJrTE2VTx?= NH;4U|FqdmirYnn0d{Bo\W2laYThZolv\S2rbnT1Z4VlKGG3dH;wbIFogQ>? NHnXWo0zPDB4OUC2PS=>
WERI MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIPJcnF,OTBizsznM41t NVnxTGdsTE2VTx?= NVe1XVBscW6qaXLpeJMh\3Kxd4ToJI9nKHKndHnuc4Jt[XO2b33hJINmdGy| MVSyOFg{PzF2Mh?=
WERI NWq5UpY1TnWwY4Tpc44h[XO|YYm= MoTrglExKM7:Zz;tcC=> NYHyUFZETE2VTx?= M4r6[YJtd2OtczDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9v M{jVWVI1QDN5MUSy
Y-79 M2ezfmZ2dmO2aX;uJIF{e2G7 MYf+NVAh|rypL33s NV:zcIIzTE2VTx?= M3fkZ4Jtd2OtczDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9v M1jKU|I1QDN5MUSy
Y-79 MojBSpVv[3Srb36gZZN{[Xl? NXTQU5NChjFyIN88[{9udA>? MWLEUXNQ NIfGV3li\m[nY4TzJHlCWC2WRVHEJJBzd3SxLX;uZ49o\W6nIIDheIh4[Xl? M3LBTVI1QDN5MUSy
Y-79 MmjuSpVv[3Srb36gZZN{[Xl? MnuxglExKM7:Zz;tcC=> MoTNSG1UVw>? NYnrN|NI\G:5bj3y[Yd2dGG2ZYOgdIx2emmyb4TlcoN6KG2jcnvldkBQS1RvNB?= M1zmdFI1QDN5MUSy

... 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 Active, not recruiting Age-related Macular Degeneration; Polypoidal Choroidal Vasculopathy (PCV) Novartis Pharmaceuticals|Novartis August 7, 2013 Phase 4
NCT03033225 Active, not recruiting Pancreatic Cancer Non-Resectable Mayo Clinic January 2017 Phase 2
NCT02939274 Recruiting Metastatic Breast Cancer Rogers Sciences Inc. October 2016 Phase 2
NCT02702700 Recruiting Pleural Effusion, Malignant Centre Hospitalier Universitaire Vaudois January 2016 Phase 1
NCT02495181 Recruiting Polypoidal Choroidal Vasculopathy Association for Innovation and Biomedical Research on Light and Image|European Vision Institute Clinical Research Network January 2016 Phase 4
NCT02457026 Withdrawn Neovascular Age-related Macular Degeneration Duke University|Bausch & Lomb Incorporated January 2016 --

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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