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CBR-470-1

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Catalog No. T40063Cas No. 2416095-06-0

CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.

CBR-470-1

CBR-470-1

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Purity: 98.87%
Catalog No. T40063Cas No. 2416095-06-0
CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.
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2 mg$35In StockIn 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:98.87%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.
Targets&IC50
ARE-LUC:962 nM (EC50)
In vitro
In IMR32 cells, CBR-470-1, when applied for 24 hours at concentrations ranging from 0.01 to 10 μM, demonstrates an EC50 of 962 nM in the ARE-LUC reporter assay[1].Furthermore, CBR-470-1 induces a dose- and time-dependent accumulation of Nrf2 protein in IMR32 cells when administered at concentrations between 0.5 and 20 μM over a period of 1 to 24 hours[1].In SH-SY5Y cells, a 4-hour treatment with CBR-470-1 at 10 μM activates the Nrf2 signaling cascade[2].Moreover, a 2-hour exposure to CBR-470-1 at 10 μM inhibits MPP+-induced oxidative injury in SH-SY5Y neuronal cells[2].
Chemical Properties
Molecular Weight365.9
FormulaC14H20ClNO4S2
Cas No.2416095-06-0
SmilesS(=O)(=O)([C@@H]1[C@@H](NCC(C)C)CS(=O)(=O)C1)C2=CC=C(Cl)C=C2
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: 100 mg/mL (273.3 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.66 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 mM2.7330 mL13.6649 mL27.3299 mL136.6494 mL
5 mM0.5466 mL2.7330 mL5.4660 mL27.3299 mL
10 mM0.2733 mL1.3665 mL2.7330 mL13.6649 mL
20 mM0.1366 mL0.6832 mL1.3665 mL6.8325 mL
50 mM0.0547 mL0.2733 mL0.5466 mL2.7330 mL
100 mM0.0273 mL0.1366 mL0.2733 mL1.3665 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:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% 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

Keywords

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