Art. -Nr.: HY-123481

JNJ-42253432

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JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK_i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.

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Reinheit: 98.15%
CAS. Nr.: 1428327-35-8
Formel: C₂₈H₃₈N₄O
Molecular Weight:446.63

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

JNJ-42253432 Chemical Structure

CAS. Nr.: 1428327-35-8

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Biologische Aktivität
- Beschreibung
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK_i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively^[1].

Alle P2X Receptor Isoform-spezifische Produkte anzeigen :

In Vivo

When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED₅₀ of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED₅₀ of 10 mg/kg for SERT occupancy^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1428327-35-8
Appearance Solid
Molecular Weight 446.63
Formel C₂₈H₃₈N₄O
Color White to off-white
SMILES

O=C(NCC1(CCCCC1)N2CCN(CC2)C3=CC=CC=C3)C4=CC=CC5=C4CCN(C5)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (223.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2390 mL

11.1949 mL

22.3899 mL

5 mM

0.4478 mL

2.2390 mL

4.4780 mL

10 mM

0.2239 mL

1.1195 mL

2.2390 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Brian Lord, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2390 mL	11.1949 mL	22.3899 mL	55.9747 mL
	5 mM	0.4478 mL	2.2390 mL	4.4780 mL	11.1949 mL
	10 mM	0.2239 mL	1.1195 mL	2.2390 mL	5.5975 mL
	15 mM	0.1493 mL	0.7463 mL	1.4927 mL	3.7316 mL
	20 mM	0.1119 mL	0.5597 mL	1.1195 mL	2.7987 mL
	25 mM	0.0896 mL	0.4478 mL	0.8956 mL	2.2390 mL
	30 mM	0.0746 mL	0.3732 mL	0.7463 mL	1.8658 mL
	40 mM	0.0560 mL	0.2799 mL	0.5597 mL	1.3994 mL
	50 mM	0.0448 mL	0.2239 mL	0.4478 mL	1.1195 mL
	60 mM	0.0373 mL	0.1866 mL	0.3732 mL	0.9329 mL
	80 mM	0.0280 mL	0.1399 mL	0.2799 mL	0.6997 mL
	100 mM	0.0224 mL	0.1119 mL	0.2239 mL	0.5597 mL

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JNJ-42253432

Bioactive Compound Library Max

Bioactive Compound Library

Membrane Transporter/Ion Channel Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle P2X Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JNJ-42253432

Bioactive Compound Library Max

Bioactive Compound Library

Membrane Transporter/Ion Channel Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle P2X Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JNJ-42253432 Related Classifications

HY-123481 Related Classifications