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L-168049

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Catalog No. T22893Cas No. 191034-25-0
Alias L-168,049

L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively.

L-168049

L-168049

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Catalog No. T22893Alias L-168,049Cas No. 191034-25-0
L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$39In StockIn Stock
5 mg$89In StockIn Stock
10 mg$147In StockIn Stock
25 mg$313In StockIn Stock
50 mg$562In StockIn Stock
100 mg$843In StockIn Stock
1 mL x 10 mM (in DMSO)$125In 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:>99.99%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively.
Targets&IC50
Glucagon receptor (murine):63 nM (IC50), Glucagon receptor (human):3.7 nM (IC50), Glucagon receptor (canine):60 nM (IC50)
In vitro
In Chinese hamster ovary cells expressing the human glucagon receptor, L-168049 increases the apparent EC50 of glucagon-stimulated adenylate cyclase and decreases maximal glucagon stimulation with a Kb of 25 nM[1]. L-168049 blocks glucagon-stimulated cAMP formation in mouse liver membrane and inhibits glucagon (100 pM)-stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor with IC50 of 41 nM [3].
In vivo
In the liver of L-G6pc-/- mice, L-168049 (50 mg/kg body; p.o.) reduces Pck1 mRNA expression by half within 6 hours. L-168049 prevents the increase in G6pc expression in the kidney and gut [2].
SynonymsL-168,049
Chemical Properties
Molecular Weight467.79
FormulaC24H20BrClN2O
Cas No.191034-25-0
SmilesCCCOc1ccc(Br)cc1-c1cc([nH]c1-c1ccncc1)-c1ccc(Cl)cc1
Relative Density.1.367g/cm3
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
Ethanol: 3.4 mM, Sonication is recommended.
DMSO: insoluble
Solution Preparation Table
Ethanol
1mg5mg10mg50mg
1 mM2.1377 mL10.6886 mL21.3771 mL106.8856 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:
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