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KB-74935

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Catalog No. T32368Cas No. 946398-78-3
Alias KB 74935

KB-74935 is an enzyme inhibitor and a mineralocorticoid receptor antagonist used to treat cholesterol, hypolipidemia, neurological disorders, and Alzheimer's disease.

KB-74935

KB-74935

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Purity: 99.4%
Catalog No. T32368Alias KB 74935Cas No. 946398-78-3
KB-74935 is an enzyme inhibitor and a mineralocorticoid receptor antagonist used to treat cholesterol, hypolipidemia, neurological disorders, and Alzheimer's disease.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$256In StockIn Stock
5 mg$525In StockIn Stock
10 mg$659In StockIn Stock
25 mg$783In StockIn Stock
50 mg$903In StockIn Stock
100 mg$1,050In StockIn Stock
200 mg$1,230-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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:99.4%
Appearance:Solid
Color:White
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Product Introduction

KB-74935 AI Summary
KB-74935 exhibits potent inhibition of human and mouse 11betaHSD1 enzyme with an IC50 value of 10.0 nM. It has good metabolic stability in both mouse and human liver microsomes, with a half-life of more than 0.5 hours. In vivo studies in mice show significant inhibition of 11betaHSD1 in epididymal fat tissue and liver, with inhibition percentages of 80.0% and 95.0% respectively. The compound displays favorable pharmacokinetic profiles in mice, including a Tmax of 4.0 hours, Cmax of 2996.58 nM, clearance of 5.0 mL/min/kg, volume of distribution at steady state (Vdss) of 2.6 L/kg, and half-lives ranging from 7.2 to 7.3 hours. Its oral bioavailability in mice is 50.0% at a dose of 10 mg/kg. Drug uptake measurements indicate tissue-specific distribution and accumulation in mouse serum, liver, and fat tissues. Additionally, KB-74935 shows variable intrinsic clearance rates in human liver microsomes (ranging from less than 3 to greater than 150 µL/min/mg) and a clearance rate of 63.1 µL/min per 10^6 cells in rat hepatocytes, suggesting metabolic activities in both human and rat liver cells..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
KB-74935 is an enzyme inhibitor and a mineralocorticoid receptor antagonist used to treat cholesterol, hypolipidemia, neurological disorders, and Alzheimer's disease.
SynonymsKB 74935
Chemical Properties
Molecular Weight479.88
FormulaC19H18ClF4N3O3S
Cas No.946398-78-3
SmilesC(F)(F)(F)C1=C(C=CC(F)=C1)N2C[C@@H](C)N(S(=O)(=O)C3=C(Cl)C=C(C(N)=O)C=C3)CC2
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: 4.8 mg/mL (10 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0839 mL10.4193 mL20.8385 mL104.1927 mL
5 mM0.4168 mL2.0839 mL4.1677 mL20.8385 mL
10 mM0.2084 mL1.0419 mL2.0839 mL10.4193 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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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