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 NF7UTYFHfW6ldHnvckBie3OjeR?= M1GxcZ4yODBibnevcWw> NVPVbIhyTE2VTx?= NUm1e2x4cW6lcnXhd4V{KESQQTDmdoFodWWwdHH0bY9vKGyndnXsdy=> M2jCcVExPjB5N{Gw
HL-60 MUPjfZRwfG:6aXPpeJkh[XO|YYm= MmPHglExOCCwZz;tUC=> NIT2TnlFVVOR M1O4N4lvcGmkaYTzJINmdGxidnnhZoltcXS7 MnHBNVA3ODd5MUC=
Jurkat NWnMWVlCSXCxcITvd4l{KGG|c3H5 MofmglI5OCCwTR?= M2r1SGROW09? MUfpcoR2[2W|IHGgRoNtNTJvZHXw[Y5l\W62IHHwc5B1d3Orcx?= NYC2[mhZOTF{NEW0NVU>
RIF-1 MXHGeY5kfGmxbjDhd5NigQ>? MXSxJO69\y:vbB?= MULEUXNQ MY\k[YNz\WG|ZYOgc5h6\2WwIHPvcpN2dXC2aX;u NHPvXnMyOjZzNUexPC=>
RIF-1 MljkZ5l1d3SxeHnjbZR6KGG|c3H5 MlvJNUDPxGdxbXy= NW\hcFY2TE2VTx?= Mney[IVkemWjc3WgeI8hOjBiwsGgOUUh[2WubDDzeZJ3cX[jbB?= MUixNlYyPTdzOB?=
SVEC4-10 MVvGeY5kfGmxbjDhd5NigQ>? M{jLNlIxOCCwZz;tcC=> NW\aUIV3TE2VTx?= NGLROVNqdmS3Y3XzJI1q[3KxdIXieYxmKGSncH;sfY1memm8YYTpc44> MXWxOlQ3PzFyNh?=
SVEC4-10 M3\1SmZ2dmO2aX;uJIF{e2G7 M3zOPFIxOCCwZz;tcC=> Mof3SG1UVw>? NXnEV4FvcW6mdXPld{B{fHKnc4OgZYN1cW5iZnni[ZIh\m:{bXH0bY9v M4[4elE3PDZ5MUC2
ARPE-19 M3yzOoN6fG:2b4jpZ4l1gSCjc4PhfS=> NHnueVV,OC5zIN88[{9udA>? NH;WZ4tFVVOR NH;MZ25{cG:5czDhJIRwe2VvZHXw[Y5l\W62IITvfIlkcXS7 MlXxNVY6QDd7MEW=
ARPE-19 NUP5bYJSTnWwY4Tpc44h[XO|YYm= MX:wMlAyKM7:Zz;tcC=> MX;EUXNQ M2\GOIlv[3KnYYPld{BXTUeIIHHu[EBz\WS3Y3XzJHBGTEZiZYjwdoV{e2mxbh?= MnyxNVY6QDd7MEW=
Y-79 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH3NeIt,OSEQvHevcYw> NFn2VYpFVVOR NED6bphl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u MUSxPFU4QTd4NB?=
WERI-Rb1 MkfrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlvrglEh|rypL33s NYPlTHdpTE2VTx?= NFrzRXVl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u MkX0NVg2Pzl5NkS=
RB247C3 NIfWZlJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWX+NUDPxGdxbXy= NFi4WIhFVVOR NFeyVJpl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u M2rWTVE5PTd7N{[0
RB355 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{DQWJ4yKM7:Zz;tcC=> M3HCbmROW09? NXrvPZdL\GWlcnXhd4V{KHKndHnuc4Jt[XO2b33hJINmdGxicILvcIln\XKjdHnvci=> NUP1T3cxOTh3N{m3OlQ>
RB383 M3y1T2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1O3SZ4yKM7:Zz;tcC=> M1XNOWROW09? MlTP[IVkemWjc3XzJJJmfGmwb3LsZZN1d22jIHPlcIwheHKxbHnm[ZJifGmxbh?= MX:xPFU4QTd4NB?=
hFibro MWLjfZRwfG:6aXPpeJkh[XO|YYm= MYKwMlUhyrWpL33s NFGxdHRFVVOR NFHwNoxl\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEi2MFUm NGLGNoczOzR2MUGxOC=>
pTMC MmnkZ5l1d3SxeHnjbZR6KGG|c3H5 NIm1VFkxNjViwsXnM41t NYq2dY9UTE2VTx?= M3e5W4Rm[3KnYYPld{B3cWGkaXzpeJkh[nliOUKuPUU> MnXpNlM1PDFzMUS=
hTMC Mn\2Z5l1d3SxeHnjbZR6KGG|c3H5 MlPBNE42KML3Zz;tcC=> NEG4NW1FVVOR Ml\C[IVkemWjc3XzJJZq[WKrbHn0fUBjgSB6OD65KS=> M1v3cFI{PDRzMUG0
ARPE-19 M3Xhe4N6fG:2b4jpZ4l1gSCjc4PhfS=> MmnyNE42KML3Zz;tcC=> M3T6fGROW09? MYrk[YNz\WG|ZYOgeoli[mmuaYT5JIJ6KDV3LkWl MXKyN|Q1OTFzNB?=
Panc-1 NV3WZYFoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2TQcFExKM7:TR?= MnjzSG1UVw>? NHi2fndqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NXL0WZNOOjRyNkmwOlk>
MIA PaCa-2 NULGOWNST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkXONVAh|ryP MU\EUXNQ NXr3bGt3cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NFT5TVkzPDB4OUC2PS=>
BxPC-3 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH7jVJIyOCEQvF2= MojSSG1UVw>? MVjpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZ49ueGyndHXsfS=> NITJTXozPDB4OUC2PS=>
SU86.86 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmPhNVAh|ryP M4\uU2ROW09? Mlf0bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJINwdXCuZYTlcJk> NUD6NJRuOjRyNkmwOlk>
MCF-7 MYXBeZRweGijZ4mgZZN{[Xl? NIDtXFAyOCEQvF2= M2XzfGROW09? MlrLbY5pcWKrdIOg[4Vu[2m2YXLpcoUucW6mdXPl[EBifXSxcHjh[5k> MU[yOFA3QTB4OR?=
WERI Mn;hS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYX+NVAh|rypL33s NWXXTGhVTE2VTx?= M{[5colvcGmkaYTzJIdzd3e2aDDv[kBz\XSrbn;icIF{fG:vYTDj[Yxtew>? MU[yOFg{PzF2Mh?=
WERI NF;YNW9HfW6ldHnvckBie3OjeR?= Ml;6glExKM7:Zz;tcC=> MnzPSG1UVw>? M4L6V4Jtd2OtczDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9v NUTRdIxiOjR6M{exOFI>
Y-79 NXTCWVMxTnWwY4Tpc44h[XO|YYm= M1PXdp4yOCEQvHevcYw> MkLXSG1UVw>? NFfzcWVjdG:la4OgZ4VtdCCleXPs[UBxem:pcnXzd4lwdg>? M1nOTlI1QDN5MUSy
Y-79 NHHOfWxHfW6ldHnvckBie3OjeR?= NEDnb5R,OTBizsznM41t Mn3OSG1UVw>? M2TSU4Fn\mWldIOgXWFRNVSHQVSgdJJwfG9vb37jc4dmdmVicHH0bJdigQ>? NWXqeWg1OjR6M{exOFI>
Y-79 NV\tN4dtTnWwY4Tpc44h[XO|YYm= MlPKglExKM7:Zz;tcC=> MW\EUXNQ M17uToRwf25vcnXneYxifGW|IIDseZJqeG:2ZX7jfUBu[XKtZYKgU2NVNTR? NHjVV|gzPDh|N{G0Ni=>

... 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
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