Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Verteporfin [129497-78-5]

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Referência NB-64-19834-2mg

Tamanho : 2mg

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Verteporfin

(Synonyms: CL 318952, BPD-MA) Copy Product Info

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Synonyms: CL 318952, BPD-MA

Catalog No. T3112 Copy Product Info

Purity: 99.82%

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Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.

Cas No. 129497-78-5

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.82%

Color:Black

Product Introduction

Bioactivity

Description	Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.
Targets & IC50	OMM1 cells:5.89 μM, Mel 270 cells:6.43 μM, Omm 2.3 cells:7.27 μM
In vitro	Verteporfin metabolizes into a less active form within the body and is rapidly cleared, primarily excreted via feces and to a lesser extent through urine. Its therapy is effective and selectively prevents fluorescein dye leakage from choroidal neovascularization (CNV) induced in experimental monkeys. Verteporfin quickly accumulates in the choroidal vasculature, retinal pigment epithelium (RPE), and photoreceptors of established rabbit eyes. Upon intravenous injection in mice, peak tissue levels of Verteporfin are reached within 3 hours, followed by a rapid decline within 24 hours.
In vivo	Verteporfin forms a complex with LDL, which may be taken up by proliferating cells (e.g., neovascular endothelial cells) through LDL receptors or endocytosis. The therapy with Verteporfin achieves complete vascular occlusion through thrombosis in the vascular channels following selective endothelial damage. As shown by optical and electron microscopy, Verteporfin therapy selectively induces occlusion in regenerating and detached choroidal capillaries, without altering the overlying photoreceptors or ganglion cells. Verteporfin rapidly exhibits apoptotic changes in conjunction with light, as demonstrated by the activation of caspase-3 and caspase-9 and the cleavage of PARP in HL-60 cells, changes that are inhibited by the broad-spectrum caspase inhibitor ZVAD.fmk.
Synonyms	CL 318952, BPD-MA
Kinase Assay	Cells (5 × 103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader.
Cell Research	Verteporfin is dissolved in DMSO. PDX cells co-cultured with S17 cells are treated with 16 combinations of verteporfin (60 nM, 120 nM, 180 nM, and 240 nM) and dasatinib (12 nM, 24 nM, 36 nM, and 48 nM). The viabilities of cells treated with each combination are measured after 48 h using FACS Aria flow cytometer. In order to estimate drug interaction between verteporfin and dasatinib, a normalized isobologram and fraction affectedcombination index (CI) plot are made using CompuSyn software. CI values greater than 1.0 indicated antagonistic effects, equal to 1.0 additive effects, and below 1.0 synergistic effects.

Chemical Properties

Molecular Weight	718.79
Formula	C₄₁H₄₂N₄O₈
Cas No.	129497-78-5
Smiles	COC(=O)CCc1c(C)c2cc3[nH]c(cc4nc(cc5[nH]c(cc1n2)c(CCC(O)=O)c5C)[C@]1(C)[C@H](C(=O)OC)C(=CC=C41)C(=O)OC)c(C)c3C=C
Relative Density.	no data available

Storage & Solubility Information

Storage

Keep away from direct sunlight,Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 130 mg/mL (180.86 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (6.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.3912 mL	6.9561 mL	13.9123 mL	69.5613 mL
5 mM	0.2782 mL	1.3912 mL	2.7825 mL	13.9123 mL
10 mM	0.1391 mL	0.6956 mL	1.3912 mL	6.9561 mL
20 mM	0.0696 mL	0.3478 mL	0.6956 mL	3.4781 mL
50 mM	0.0278 mL	0.1391 mL	0.2782 mL	1.3912 mL
100 mM	0.0139 mL	0.0696 mL	0.1391 mL	0.6956 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

Yes-associated proteinYAPVerteporfinVDAInhibitorinhibitCL-318952CL318952AutophagyApoptosis

Related Tags: Verteporfin chemical structure | Verteporfin in vivo | Verteporfin in vitro | Verteporfin formula | Verteporfin molecular weight