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VU0134992

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Catalog No. T8372Cas No. 755002-90-5
Alias VU 0134992

VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM

VU0134992

VU0134992

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Purity: 99.86%
Catalog No. T8372Alias VU 0134992Cas No. 755002-90-5
VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$31In StockIn Stock
10 mg$54In StockIn Stock
25 mg$106In StockIn Stock
50 mg$179In StockIn Stock
100 mg$297In StockIn Stock
1 mL x 10 mM (in DMSO)$44In 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:99.86%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
VU0134992 is an Kir4.1 blocker with an IC50 value of 0.97 μM
Targets&IC50
KIR4.1:0.97 µM 
In vitro
VU0134992 inhibits Kir4.1 with an IC50 value of 0.97 μM and is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50 = 9 μM) at -120 mV.?In thallium (Tl+) flux assays, VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2;?is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1;?and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2.
In vivo
VU0134992 displayed a large free unbound fraction (fu) in rat plasma (fu = 0.213).?Consistent with the known role of Kir4.1 in renal function, oral dosing of VU0134992 led to a dose-dependent diuresis, natriuresis, and kaliuresis in rats.
SynonymsVU 0134992
Chemical Properties
Molecular Weight411.38
FormulaC20H31BrN2O2
Cas No.755002-90-5
SmilesN(C(COC1=C(Br)C=C(C(C)C)C=C1)=O)C2CC(C)(C)NC(C)(C)C2
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 60 mg/mL (145.85 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4308 mL12.1542 mL24.3084 mL121.5421 mL
5 mM0.4862 mL2.4308 mL4.8617 mL24.3084 mL
10 mM0.2431 mL1.2154 mL2.4308 mL12.1542 mL
20 mM0.1215 mL0.6077 mL1.2154 mL6.0771 mL
50 mM0.0486 mL0.2431 mL0.4862 mL2.4308 mL
100 mM0.0243 mL0.1215 mL0.2431 mL1.2154 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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μL
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

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