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BI 689648

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Catalog No. T14664Cas No. 1633009-87-6

BI 689648 is a highly selective inhibitor of aldosterone synthase(CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively).

BI 689648

BI 689648

😃Good
Catalog No. T14664Cas No. 1633009-87-6
BI 689648 is a highly selective inhibitor of aldosterone synthase(CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$9856-8 weeks6-8 weeks
50 mg$1,2806-8 weeks6-8 weeks
100 mg$1,9406-8 weeks6-8 weeks
1 mL x 10 mM (in DMSO)$2726-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
BI 689648 is a highly selective inhibitor of aldosterone synthase(CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively).
Targets&IC50
CYP11B2:2.1 nM, CYP11B1:310 nM
In vitro
In comparison with FADs and LCI699, BI 689648 exhibits remarkable selectivity in vitro, demonstrating an IC50 value of 2.1 nM for CYP11B2 and a selectivity factor of 149 over CYP11B1. Meanwhile, FAD286 presents a comparable IC50 value for CYP11B2 at 2.5 nM, but its higher efficacy against CYP11B1 (94 nM) yields a relatively lower selectivity factor of 38, which is about fourfold lesser than that of BI 689648[1].
In vivo
After oral administration in cyno monkeys, BI 689648 (5 mg/kg) achieves a peak plasma concentration of ~500 nM. BI 689648 minimally impacts 11-DC, but only at very high plasma concentrations (~10 μM)[1]. For BI 689648 (aldosterone EC50 = 2 nM), significant changes in 11-DOC are observed at plasma concentrations >2000 nM or >1000-fold its aldosterone EC50, whereas FAD286 exhibits a window of ~100-fold.
Chemical Properties
Molecular Weight298.34
FormulaC16H18N4O2
Cas No.1633009-87-6
SmilesCOCc1cncc(c1)-c1cnc2N(CCCc2c1)C(N)=O
Relative Density.1.260 g/cm3 (Predicted)
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: 30 mg/mL (100.56 mM), Sonication and heating are recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (6.7 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 mM3.3519 mL16.7594 mL33.5188 mL167.5940 mL
5 mM0.6704 mL3.3519 mL6.7038 mL33.5188 mL
10 mM0.3352 mL1.6759 mL3.3519 mL16.7594 mL
20 mM0.1676 mL0.8380 mL1.6759 mL8.3797 mL
50 mM0.0670 mL0.3352 mL0.6704 mL3.3519 mL
100 mM0.0335 mL0.1676 mL0.3352 mL1.6759 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

You can also refer to dose conversion for different animals. More Dose Conversion

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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