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JNJ-42253432

Name: JNJ-42253432
Brand: TargetMol
SKU: T27683
Price: 71 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T27683Cas No. 1428327-35-8

JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.

JNJ-42253432

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Purity: 99.98%

Catalog No. T27683Cas No. 1428327-35-8

JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$71	In Stock	In Stock
5 mg	$178	In Stock	In Stock
10 mg	$269	In Stock	In Stock
25 mg	$418	In Stock	In Stock
50 mg	$562	In Stock	In Stock
100 mg	$743	In Stock	In Stock
200 mg	$987	-	In Stock
1 mL x 10 mM (in DMSO)	$203	In Stock	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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Batch Information

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Purity:99.98%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

JNJ-42253432 AI Summary

JNJ-42253432 exhibits a range of bioactivities and pharmacokinetic characteristics. It shows moderate inhibition of rat nACHR with an IC50 of 910 nM and significant inhibition of human dopamine transporter with an IC50 of 290 nM. At a concentration of 1 μM, it inhibits rat nACHR by 54% relative to control, and human dopamine transporter by 93%. It also targets the human NK2 receptor, demonstrating 68% inhibition at 1 μM. For P2X7 receptors, JNJ-42253432 acts as an antagonist, displaying an IC50 of 199.53 nM in human whole blood, 39.81 nM in human PBMC, 79.43 nM in mouse receptors, and 15.85 nM in rat receptors. It also inhibits the human recombinant P2X7 receptor in 1321N1 cells with an IC50 of 19.95 nM. The compound binds with high affinity to the human serotonin transporter, displacing [3H]-Citalopram with a Ki of 15.85 nM. In terms of pharmacokinetics, JNJ-42253432 exhibits a high intrinsic clearance rate of 200 mL.min^-1.kg^-1 in rat liver microsomes. Its apparent permeability across the basolateral to apical side in MDCK-MDR1 cells is low, with a Papp value of 0.25 x10^-6 cm/s, and it shows a slight efflux effect with an efflux ratio of 1.1 in MDCK2-MDR1 cells..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.
Targets&IC50	P2X7:9.1(pKi, rat), P2X7:7.9(pKi, human)

Chemical Properties

Molecular Weight	446.63
Formula	C₂₈H₃₈N₄O
Cas No.	1428327-35-8
Smiles	CN1CCc2c(C1)cccc2C(=O)NCC1(CCCCC1)N1CCN(CC1)c1ccccc1
Relative Density.	1.130 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: 90 mg/mL (201.51 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.39 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	2.2390 mL	11.1949 mL	22.3899 mL	111.9495 mL
5 mM	0.4478 mL	2.2390 mL	4.4780 mL	22.3899 mL
10 mM	0.2239 mL	1.1195 mL	2.2390 mL	11.1949 mL
20 mM	0.1119 mL	0.5597 mL	1.1195 mL	5.5975 mL
50 mM	0.0448 mL	0.2239 mL	0.4478 mL	2.2390 mL
100 mM	0.0224 mL	0.1119 mL	0.2239 mL	1.1195 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