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voxelotor

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Catalog No. T7581Cas No. 1446321-46-5
Alias GBT 440

Voxelotor (GBT 440) is a novel hemoglobin S (HbS) polymerization inhibitor primarily used for the treatment of sickle cell disease (SCD) and a cytochrome P450 3A4 inhibitor. Voxelotor targets and covalently binds to the N-terminal valine of the HbS alpha chain, thereby stabilizing sickle cell hemoglobin (HbS).

voxelotor

voxelotor

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Purity: 99.94%
Catalog No. T7581Alias GBT 440Cas No. 1446321-46-5
Voxelotor (GBT 440) is a novel hemoglobin S (HbS) polymerization inhibitor primarily used for the treatment of sickle cell disease (SCD) and a cytochrome P450 3A4 inhibitor. Voxelotor targets and covalently binds to the N-terminal valine of the HbS alpha chain, thereby stabilizing sickle cell hemoglobin (HbS).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$42In StockIn Stock
10 mg$67In StockIn Stock
25 mg$122In StockIn Stock
50 mg$198In StockIn Stock
100 mg$369-In Stock
200 mg$549-In Stock
1 mL x 10 mM (in DMSO)$46In 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:99.94%
Color:White
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Product Introduction

Bioactivity
Description
Voxelotor (GBT 440) is a novel hemoglobin S (HbS) polymerization inhibitor primarily used for the treatment of sickle cell disease (SCD) and a cytochrome P450 3A4 inhibitor. Voxelotor targets and covalently binds to the N-terminal valine of the HbS alpha chain, thereby stabilizing sickle cell hemoglobin (HbS).
Targets&IC50
ERG (human):> 10 μM
In vitro
METHODS: Voxelotor (3-30 µmol/L) was incubated with hemoglobin (25 µmol/L) in TES or saline buffer at 37 ℃ for 45 min, and changes in the binding affinity of O2 for Hb were measured using a TCS hematology analyzer.
RESULTS: Voxelotor, a small molecule that binds to the N-terminal α-chain of Hb, increases the affinity of HbS for oxygen, delays HbS polymerization in vitro and prevents erythrocyte sickling. [1]
METHODS: HepG2 cells were treated with Voxelotor (1 µg/mL) and their metabolites were analyzed by liquid chromatography, high-resolution MS and tandem MS.
RESULTS: Voxelotor can be used for the identification of phase I and phase II metabolites in vitro. [2]
In vivo
METHODS: To assess the activity and efficacy of Voxelotor, Voxelotor (100-150 mg/kg, 0.5% methylcellulose/0.5% SDS) was administered by gavage to a mouse model of SCD twice daily for 9-12 days.
RESULTS: Voxelotor reduced isolated sickle cells and prolonged erythrocyte half-life in the SCD mouse model. [1]
SynonymsGBT 440
Chemical Properties
Molecular Weight337.37
FormulaC19H19N3O3
Cas No.1446321-46-5
SmilesCC(C)n1nccc1-c1ncccc1COc1cccc(O)c1C=O
Relative Density.1.23 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 79 mg/mL (234.16 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.93 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 mM2.9641 mL14.8205 mL29.6410 mL148.2052 mL
5 mM0.5928 mL2.9641 mL5.9282 mL29.6410 mL
10 mM0.2964 mL1.4821 mL2.9641 mL14.8205 mL
20 mM0.1482 mL0.7410 mL1.4821 mL7.4103 mL
50 mM0.0593 mL0.2964 mL0.5928 mL2.9641 mL
100 mM0.0296 mL0.1482 mL0.2964 mL1.4821 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
%
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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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