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TAK-220

Name: TAK-220
Brand: TargetMol
SKU: T16973
Rating: 4.5 (1 reviews)

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Catalog No. T16973Cas No. 333994-00-6

TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5.

TAK-220

😃Good

Catalog No. T16973Cas No. 333994-00-6

TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$347	6-8 weeks	6-8 weeks
25 mg	$1,140	6-8 weeks	6-8 weeks
50 mg	$1,490	6-8 weeks	6-8 weeks
100 mg	$1,990	6-8 weeks	6-8 weeks
1 mL x 10 mM (in DMSO)	$382	6-8 weeks	6-8 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	TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5.
Targets&IC50	HIV-1 (HKW):12 nM （EC90）（in PBMCs), HIV-1 (HHA):0.55 nM （EC50）（in PBMCs), HIV-1 (HTN):0.93 nM （EC50）（in PBMCs), HIV-1 (HNK):1.7 nM （EC50）（in PBMCs), HIV-1 (KK):1.2 nM （EC50）（in PBMCs), HIV-1 (HTN):15 nM （EC90）（in PBMCs), HIV-1 (KK):12 nM （EC90）（in PBMCs), X4 HIV-1 (CTV):0.72 nM （EC50）（in PBMCs), HIV-1 (HKW):1.7 nM （EC50）（in PBMCs), HIV-1 (HNK):28 nM （EC90）（in PBMCs), HIV-1 (HHA):4 nM （EC90）（in PBMCs), RANTES-CCR5:3.5 nM （in CHO cells), MIP-1α-CCR5:1.4 nM （in CHO cells), X4 HIV-1 (CTV):5 nM （EC90）（in PBMCs)
In vitro	TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion (IC50: 0.42 nM). TAK-220 shows potent inhibitory activity against the R5 isolates, with IC50s of 3.12 nM against HIV-1 R5-08, 13.47 nM against HIV-1 R5-06, and 2.26 nM against HIV-1 R5-18. TAK-220 (>100 nM) has no toxicity in uninfected PBMCs. TAK-220 (0-1000 nM) interacts with CCR5 but not with RANTES and inhibits the CCR5-mediated Casup>2+ signaling. TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs [1][2].

Chemical Properties

Molecular Weight	553.14
Formula	C₃₁H₄₁ClN₄O₃
Cas No.	333994-00-6
Smiles	CC(=O)N1CCC(CC1)C(=O)N(CCCN1CCC(Cc2ccc(cc2)C(N)=O)CC1)c1ccc(C)c(Cl)c1
Relative Density.	1.208 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (90.39 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (4.52 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	1.8079 mL	9.0393 mL	18.0786 mL	90.3930 mL
5 mM	0.3616 mL	1.8079 mL	3.6157 mL	18.0786 mL
10 mM	0.1808 mL	0.9039 mL	1.8079 mL	9.0393 mL
20 mM	0.0904 mL	0.4520 mL	0.9039 mL	4.5197 mL
50 mM	0.0362 mL	0.1808 mL	0.3616 mL	1.8079 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