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BI 224436

Name: BI 224436
Brand: TargetMol
SKU: T14559
Rating: 4.5 (1 reviews)

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Catalog No. T14559Cas No. 1155419-89-8

BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains.

BI 224436

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Catalog No. T14559Cas No. 1155419-89-8

BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$5,130	10-14 weeks	10-14 weeks
5 mg	$9,870	10-14 weeks	10-14 weeks

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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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Product Introduction

Bioactivity

Description	BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains.
Targets&IC50	HIV-1:（EC50）15 nM
In vitro	BI 224436 exhibits over 90 μM cellular cytotoxicity and retains its antiviral efficacy with a minimal 2.1-fold reduction in the presence of 50% human serum. It possesses favorable in vitro drug-like absorption, distribution, metabolism, and excretion (ADME) characteristics, such as Caco-2 cell permeability, solubility, and minimal cytochrome P450 inhibition[1]. Moreover, BI 224436 maintains complete antiviral functionality against recombinant viruses bearing integrase strand transfer inhibitor (INSTI) resistance mutations, namely N155S, Q148H, and E92Q. Additionally, it demonstrates an additive effect when used alongside most approved antiretrovirals, including INSTIs.
In vivo	BI 224436 demonstrates favorable pharmacokinetic properties across multiple species, including rats, monkeys, and dogs. Specifically, in rats, the compound has a clearance rate of 0.7% as a percentage of hepatic flow and a bioavailability of 54%. In monkeys, the clearance rate is 23% with an 82% bioavailability, while in dogs, the clearance is 8%, with bioavailability reaching 81%[1].

Chemical Properties

Molecular Weight	442.51
Formula	C₂₇H₂₆N₂O₄
Cas No.	1155419-89-8
Smiles	Cc1nc2ccccc2c(-c2ccc3OCCc4ccnc2c34)c1[C@H](OC(C)(C)C)C(O)=O
Relative Density.	1.277 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (112.99 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (5.65 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

	1mg	5mg	10mg	50mg
1 mM	2.2598 mL	11.2992 mL	22.5984 mL	112.9918 mL
5 mM	0.4520 mL	2.2598 mL	4.5197 mL	22.5984 mL
10 mM	0.2260 mL	1.1299 mL	2.2598 mL	11.2992 mL
20 mM	0.1130 mL	0.5650 mL	1.1299 mL	5.6496 mL
50 mM	0.0452 mL	0.2260 mL	0.4520 mL	2.2598 mL
100 mM	0.0226 mL	0.1130 mL	0.2260 mL	1.1299 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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