2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. JNJ-47965567

JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.

For research use only. We do not sell to patients.

JNJ-47965567 Chemical Structure

JNJ-47965567 Chemical Structure

CAS No. : 1428327-31-4

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

JNJ-47965567 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology[1].

IC50 & Target

pKi: 7.9 (huaman P2X7), 8.7 (rat P2X7)[1]
In Vitro

JNJ-47965567 exhibits high affinity for human and rat P2X7 in membrane preparations of 1321N1 cells[1].
JNJ-47965567 does not block IL-6 and TNF-α release, under identical conditions (LPS and BZ-ATP) used for IL-1β and IL-18 release[1].
JNJ-47965567 attenuates IL-1β release with pIC50s of 6.7 ± 0.07 (human blood), 7.5 ± 0.07 (human monocytes) and 7.1 ± 0.1 (rat microglia), respectively, in native systems[1].

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

JNJ-47965567 Related Antibodies
In Vivo

JNJ-47965567 (30-100 mg/kg; s.c.) attenuates IL-1β release induced by Bz-ATP[1].
JNJ-47965567 (30 mg/kg) attenuates amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain[1].

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

Animal Model: Male Sprague Dawley rats[1]
Dosage: 30 mg/kg, 100 mg/kg
Administration: Subcutaneous injection; 30 minutes prior to Bz-ATP infusion
Result: Significantly attenuated IL-1β release at 100 mg/kg, with no effect at 30 mg/kg dose group.
Molecular Weight

488.64

Formula

C28H32N4O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CN=C1SC2=CC=CC=C2)NCC3(N4CCN(C5=CC=CC=C5)CC4)CCOCC3
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 (204.65 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 2.0465 mL 10.2325 mL 20.4650 mL
5 mM 0.4093 mL 2.0465 mL 4.0930 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.12 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.12 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

Purity: 99.77%

COA (256 KB) HNMR (287 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
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 2.0465 mL 10.2325 mL 20.4650 mL 51.1624 mL
5 mM 0.4093 mL 2.0465 mL 4.0930 mL 10.2325 mL
10 mM 0.2046 mL 1.0232 mL 2.0465 mL 5.1162 mL
15 mM 0.1364 mL 0.6822 mL 1.3643 mL 3.4108 mL
20 mM 0.1023 mL 0.5116 mL 1.0232 mL 2.5581 mL
25 mM 0.0819 mL 0.4093 mL 0.8186 mL 2.0465 mL
30 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7054 mL
40 mM 0.0512 mL 0.2558 mL 0.5116 mL 1.2791 mL
50 mM 0.0409 mL 0.2046 mL 0.4093 mL 1.0232 mL
60 mM 0.0341 mL 0.1705 mL 0.3411 mL 0.8527 mL
80 mM 0.0256 mL 0.1279 mL 0.2558 mL 0.6395 mL
100 mM 0.0205 mL 0.1023 mL 0.2046 mL 0.5116 mL
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JNJ-47965567 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-479655671428327-31-4JNJ47965567JNJ 47965567P2X ReceptorP2XRsP2X7neuropathicpainInhibitorinhibitorinhibit

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