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Pifithrin-β hydrobromide

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Catalog No. T3637Cas No. 511296-88-1
Alias Pifithrin-β, PFT-β, PFT β (hydrobromide), Cyclic Pifithrin-α hydrobromide, Cyclic PFT-α

Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).

Pifithrin-β hydrobromide

Pifithrin-β hydrobromide

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🥰Excellent
Purity: 99.74%
Catalog No. T3637Alias Pifithrin-β, PFT-β, PFT β (hydrobromide), Cyclic Pifithrin-α hydrobromide, Cyclic PFT-αCas No. 511296-88-1
Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$34In StockIn Stock
5 mg$51In StockIn Stock
10 mg$85In StockIn Stock
25 mg$153In StockIn Stock
50 mg$223In StockIn Stock
100 mg$332In StockIn Stock
1 mL x 10 mM (in DMSO)$53In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.74%
Color:White
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Product Introduction

Bioactivity
Description
Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).
Targets&IC50
p53:23 μM(EC50)
In vitro
PFTα molecule could not take a planar conformation required for AhR activation whereas Pifithrin-β hydrobromide showed a conformation similar to those of the prototypical AhR ligand β-naphthoflavone. In both cell lines, PFTα and Pifithrin-β hydrobromide provoked different responses related with AhR activation. However, when cyclization of PFTα to Pifithrin-β hydrobromide was hampered by acetylation of the exocyclic nitrogen, all these responses were not observed. These results lead to the conclusion that the activation of the AhR is probably caused by Pifithrin-β hydrobromide instead of PFTα.
SynonymsPifithrin-β, PFT-β, PFT β (hydrobromide), Cyclic Pifithrin-α hydrobromide, Cyclic PFT-α
Chemical Properties
Molecular Weight349.29
FormulaC16H17BrN2S
Cas No.511296-88-1
SmilesBr.Cc1ccc(cc1)-c1cn2c3CCCCc3sc2n1
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 13.89 mg/mL (39.77 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.86 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
1mg5mg10mg50mg
1 mM2.8630 mL14.3148 mL28.6295 mL143.1475 mL
5 mM0.5726 mL2.8630 mL5.7259 mL28.6295 mL
10 mM0.2863 mL1.4315 mL2.8630 mL14.3148 mL
20 mM0.1431 mL0.7157 mL1.4315 mL7.1574 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
1 Enter information below:
mg/kg
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2 Enter the in vivo formulation:
% DMSO
%
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% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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