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PB28 dihydrochloride

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Catalog No. T23122Cas No. 172907-03-8
Alias PB 28 dihydrochloride

PB28 dihydrochloride is a selective and potent sigma 2 (σ2) receptor agonist and σ1 receptor antagonist with anti-SARS-CoV-2 activity and anti-tumor activity, which inhibits cell proliferation and invasion and suppresses SKF by modulating the PI3K-AKT-mTOR signaling pathway in renal cancer. It inhibits cell proliferation and invasion by regulating the PI3K-AKT-mTOR signaling pathway in renal cancer, inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells, and induces non-caspase-dependent apoptosis.

PB28 dihydrochloride

PB28 dihydrochloride

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Purity: 99.97%
Catalog No. T23122Alias PB 28 dihydrochlorideCas No. 172907-03-8
PB28 dihydrochloride is a selective and potent sigma 2 (σ2) receptor agonist and σ1 receptor antagonist with anti-SARS-CoV-2 activity and anti-tumor activity, which inhibits cell proliferation and invasion and suppresses SKF by modulating the PI3K-AKT-mTOR signaling pathway in renal cancer. It inhibits cell proliferation and invasion by regulating the PI3K-AKT-mTOR signaling pathway in renal cancer, inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells, and induces non-caspase-dependent apoptosis.
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5 mg$399-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.97%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PB28 dihydrochloride is a selective and potent sigma 2 (σ2) receptor agonist and σ1 receptor antagonist with anti-SARS-CoV-2 activity and anti-tumor activity, which inhibits cell proliferation and invasion and suppresses SKF by modulating the PI3K-AKT-mTOR signaling pathway in renal cancer. It inhibits cell proliferation and invasion by regulating the PI3K-AKT-mTOR signaling pathway in renal cancer, inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells, and induces non-caspase-dependent apoptosis.
Targets&IC50
MCF-7/ADR cells:15 nM, MCF-7/ADR cells:0.17 nM (Ki), MCF-7 cells:0.28 nM (Ki), MCF-7 cells:25 nM
In vitro
PB28 dihydrochloride has a higher affinity for the σ2 receptor, with Ki values of 0.28 nM and 0.17 nM in MCF7 and MCF7 ADR cells, respectively.Accumulation of the two types of cells in the G0-G1 phase was observed after treatment of MCF7 and MCF7 ADR cells for 24-48 h at concentrations of 15-25 nM, an effect that was not affected by time and concentration changes. and concentration changes. After 2 days of incubation, PB28 dihydrochloride effectively inhibited the growth of MCF7 and MCF7 ADR cells with IC50s of 25 nM and 15 nM, respectively.This compound triggers apoptosis through a non-cysteoaspartase-dependent pathway.
In addition, PB28 dihydrochloride significantly reduced P-gp expression in a concentration- and time-dependent manner by approximately 60% in MCF7 cells and 90% in MCF7 ADR cells. PB28 dihydrochloride also exhibited significant antiproliferative toxicity in the C6 rat glioma cell line and the SK-N-SH human neuroblastoma cell line. [1]
In vivo
PB28 dihydrochloride was injected daily intraperitoneally at a concentration of 10.7 mg/mL for two weeks into C57BL/6 female mice and was shown to be effective in inhibiting tumor growth in Panc02 tumor-loaded mice. In addition, PB28 dihydrochloride significantly increased the survival rate of mice. [2]
SynonymsPB 28 dihydrochloride
Chemical Properties
Molecular Weight443.49
FormulaC24H40Cl2N2O
Cas No.172907-03-8
SmilesCOC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3.Cl.Cl
Relative Density.no data available
Storage & Solubility Information
Storagestore 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
DMSO: 4 mg/mL (9.02 mM), Sonication is recommended.
H2O: 5 mg/mL (11.27 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.25 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/H2O
1mg5mg10mg50mg
1 mM2.2548 mL11.2742 mL22.5484 mL112.7421 mL
5 mM0.4510 mL2.2548 mL4.5097 mL22.5484 mL
H2O
1mg5mg10mg50mg
10 mM0.2255 mL1.1274 mL2.2548 mL11.2742 mL

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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:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
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