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INCB 3284 dimesylate

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Catalog No. T11647Cas No. 887401-93-6

INCB 3284 dimesylate is a selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2 (IC50: 3.7 nM). It can be used in the research of acute liver failure.

INCB 3284 dimesylate

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Catalog No. T11647Cas No. 887401-93-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$185	35 days	35 days
10 mg	$563	35 days	35 days
50 mg	$2,570	35 days	35 days

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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.However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Product Introduction

Bioactivity

Description	INCB 3284 dimesylate is a selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2 (IC50: 3.7 nM). It can be used in the research of acute liver failure.
Targets&IC50	MCP-1-hCCR2:3.7 nM
In vitro	INCB 3284 causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively.INCB 3284 dimesylate is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM.?INCB 3284 also causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current.?However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM.?Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively.
In vivo	INCB 3284 effectively diminishes the ratio of phosphorylated ERK1/2 (pERK1/2) to total ERK1/2 (tERK1/2), alongside reducing G-protein signaling pathway activity and the production of proinflammatory cytokines in cortex lysates of mice treated with azoxymethane. Additionally, administered at a dosage of 1 mg/kg/day intraperitoneally, it alleviates liver damage and curtails microglia activation in azoxymethane (AOM)-treated mice through the inhibition of CCR2.

Chemical Properties

Molecular Weight	712.76
Formula	C₂₈H₃₉F₃N₄O₁₀S₂
Cas No.	887401-93-6
Smiles	CS(=O)(O)=O.O[C@]1(C2=CN=C(OC)C=C2)CC[C@](N3C[C@@H](CC3)NC(CNC(C4=CC(C(F)(F)F)=CC=C4)=O)=O)([H])CC1.CS(=O)(O)=O
Relative Density.	no data available

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: 83.3 mg/mL (116.87 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4030 mL	7.0150 mL	14.0300 mL	70.1498 mL
5 mM	0.2806 mL	1.4030 mL	2.8060 mL	14.0300 mL
10 mM	0.1403 mL	0.7015 mL	1.4030 mL	7.0150 mL
20 mM	0.0701 mL	0.3507 mL	0.7015 mL	3.5075 mL
50 mM	0.0281 mL	0.1403 mL	0.2806 mL	1.4030 mL
100 mM	0.0140 mL	0.0701 mL	0.1403 mL	0.7015 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