2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. JNJ-28583113

JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia.

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JNJ-28583113 Chemical Structure

JNJ-28583113 Chemical Structure

CAS No. : 2765255-93-2

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Based on 1 publication(s) in Google Scholar

JNJ-28583113 Related Antibodies

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  • Purity & Documentation

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Description

JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia[1].

IC50 & Target[1]

TRPM2

 

In Vitro

JNJ-28583113 inhibits TRPM2 in cells overexpressing chimpanzee (IC50=100 nM), rat (IC50=25 nM), and human (IC50=126 nM), respectively[1].
JNJ-28583113 (3 nM, 30 nM, and 1 μM; 200 s) exhibits electrophysical characterization in ADPR-induced currents recorded in hTRPM2-HEK-inducible cells[1].
JNJ-28583113 (10 μM; 1 h) prevents cells from H2O2 induced cell death up to 1 mM of H2O2. JNJ-28583113 (10 μM; 1 h) also protects HeLa cells from H2O2 (10 μM; 1 h) induced morphological changes[1].

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

JNJ-28583113 Related Antibodies

Western Blot Analysis[1]

Cell Line: hTRPM2-HEK cells
Concentration: 10 μM
Incubation Time: 30 min
Result: Recovered phosphorylation of GSK3α and β subunits which inhibited by H2O2 (300 μM; 10 min).
In Vivo

JNJ-28583113 (10 mg/kg, 2 ml/kg; sc; single dose) is brain penetrant, and achieves 400 ng/mL in the brain compartment[1].

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

Animal Model: Harlan Sprague Dawley Rats (400 g)[1]
Dosage: 10 mg/kg, 2 mL/kg
Administration: SC; sampled at 0.5, 2, or 6 h post dosing
Result: Quickly metabolized in the plasma, while it showed high levels in plasma and low levels in the brain.
Molecular Weight

366.38

Formula

C19H21F3N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1N=C(C2=C1CCCCC2)C3=CC=C(C(F)(F)F)C=C3)OCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (272.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7294 mL 13.6470 mL 27.2941 mL
5 mM 0.5459 mL 2.7294 mL 5.4588 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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:  2% DMSO    40% PEG300    5% Tween-80    53% Saline

    Solubility: ≥ 2 mg/mL (5.46 mM); Clear solution

  • Protocol 2

    Add each solvent one by one:  2% DMSO    98% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (5.46 mM); Clear solution

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7294 mL 13.6470 mL 27.2941 mL 68.2352 mL
5 mM 0.5459 mL 2.7294 mL 5.4588 mL 13.6470 mL
10 mM 0.2729 mL 1.3647 mL 2.7294 mL 6.8235 mL
15 mM 0.1820 mL 0.9098 mL 1.8196 mL 4.5490 mL
20 mM 0.1365 mL 0.6824 mL 1.3647 mL 3.4118 mL
25 mM 0.1092 mL 0.5459 mL 1.0918 mL 2.7294 mL
30 mM 0.0910 mL 0.4549 mL 0.9098 mL 2.2745 mL
40 mM 0.0682 mL 0.3412 mL 0.6824 mL 1.7059 mL
50 mM 0.0546 mL 0.2729 mL 0.5459 mL 1.3647 mL
60 mM 0.0455 mL 0.2275 mL 0.4549 mL 1.1373 mL
80 mM 0.0341 mL 0.1706 mL 0.3412 mL 0.8529 mL
100 mM 0.0273 mL 0.1365 mL 0.2729 mL 0.6824 mL
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JNJ-28583113 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-285831132765255-93-2JNJ28583113JNJ 28583113TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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