2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. JNJ-78911118

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research.

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JNJ-78911118

JNJ-78911118 Chemical Structure

CAS No. : 3106013-91-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

JNJ-78911118 Related Antibodies

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Description

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research[1].

IC50 & Target[1]

GluN2A

44 nM (IC50)

In Vitro

JNJ-78911118 (10 pM-10 μM, 2 h) displaces the GluN1/2A interface binding radioligand JNJ-74950343 in hippocampal neuron membranes in a concentration-dependent manner, and does not alter glutamate potency but reduces its efficacy against homomeric GluN1/2A receptors[1].
JNJ-78911118 (10 μM, 24-72 h) promotes neurite outgrowth and synaptogenesis in rat hippocampal neuronal cultures, significantly enhancing multiple measures of dendritic complexity after 72 h[1].
JNJ-78911118 (1-10 μM) shows less than 50 % inhibition against all targets in a custom panel of 77 ion channels, receptors, and transporters, as well as a panel of 373 kinases[1].

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

JNJ-78911118 Related Antibodies
Parmacokinetics
Species Dose Route CL Vdss AUClast MRT T1/2 Tmax F
Mice[1] 1 mg/kg i.v. 22.9 mL/min/kg 1.0 L/kg 726.5 ng·h/mL 0.8 h 0.7 h / /
Mice[1] 5 mg/kg p.o. / / 1732.0 ng·h/mL 1.3 h 0.9 h 0.3 h 47.2 %
Mice[1] 5 mg/kg s.c. / / 3521.5 ng·h/mL 1.5 h 0.9 h 0.3 h 95.7 %
Rat[1] 1 mg/kg i.v. 41.3 mL/min/kg 1.0 L/kg 404.6 ng·h/mL 0.4 h 0.6 h / /
Rat[1] 5 mg/kg i.v. / / 1459.9 ng·h/mL 1.4 h 0.7 h 0.5 h 72.2 %
Rat[1] 5 mg/kg p.o. / / 563.0 ng·h/mL 1.7 h 1.0 h 0.3 h 28.0 %
In Vivo

JNJ-78911118 (60 mg/kg, s.c., single dose) mitigates mechanical allodynia in the Complete Freund's adjuvant (CFA) (HY-153808) mouse models of inflammatory pain, prevents hippocampal long-term potentiation (LTP) in rats and increases miniature excitatory postsynaptic current (mEPSC) frequency in the rat prefrontal cortex[1].
JNJ-78911118 (50 and 250 mg/kg, p.o., twice daily for 4 days or twice on the same day) is generally well tolerated but produces dose-related haemodynamic effects in rats[1].

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

Animal Model: Male C57BL/6 N mice (8-12 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 2 days post-CFA
Result: Partly reversed CFA induced allodynia at 60 mg/kg, while Gabapentin (HY-A0057) (150 mg/kg, p.o.) completely reversed it.
Reduced tactile allodynia at 30 min and 1 h post-administration compared to controls.
Had no effect on paw withdrawal thresholds (PWTs) 24 h post-dosing.
Animal Model: Wild-type C57BL/6J and homozygous Grin2a KO mice[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 2 days post-CFA
Result: Mitigated CFA-induced allodynia in wild type mice at 30 min and 1-h post-administration.
Did not significantly reduce CFA-induced mechanical allodynia in Grin2a KO mice.
Animal Model: Male Sprague-Dawley rats (8-10 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 30 min pre-TBS
Result: Did not alter baseline synaptic transmission but completely blocked the induction of LTP by theta burst stimulation (TBS).
The population spike amplitude remained at pre-stimulation levels throughout the recording period (50-60 min post-TBS).
Animal Model: Male Sprague-Dawley rats (6-10 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose (24 h before recording)
Result: Induced a significant decrease in the inter-event interval of mEPSCs in layer 5 pyramidal neurons in rat medial prefrontal cortex.
Showed no significant changes in mEPSC amplitude.
Animal Model: Male Wistar Han rats [1]
Dosage: 50 and 250 mg/kg
Administration: p.o., twice daily for 4 days
Result: Achieved dose-dependent plasma exposures, with Cmax and AUC increasing less than dose proportionally (80 and 180 %, respectively, and Tmax occurring 1-3 h post-dose.
Minimal activity decreases or minimal hypoactivity were observed 2 h post-dose on days 1-3.
Piloerection was observed in high-dose animals on Day 1 at 3 h post-dose.
Low doses had no effect on body weight, while the high dose caused a transient 3% decrease in two animals and lower overall body weight gain in all animals.
No meaningful changes were detected in globulin, protein, albumin, chloride, calcium and potassium concentrations, cholesterol level or reticulocyte count.
Produced mild decreases in triglyceride levels.
Showed no Olney's lesions in animals.
Animal Model: Male Sprague-Dawley rats (8-10 weeks)[1]
Dosage: 50 and 250 mg/kg
Administration: p.o., twice on the same day
Result: The low dose increased heart rate and mean arterial pressure.
The high dose caused a transient decrease in heart rate (associated with reduced body temperature) and an increase in blood pressure.
Molecular Weight

419.81

Formula

C19H16ClF2N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=NC(C(NCC2=CC=CN=C2)=O)=CN=C1OCC(F)(F)C3=CC(Cl)=CC=N3
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 (238.20 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 2.3820 mL 11.9101 mL 23.8203 mL
5 mM 0.4764 mL 2.3820 mL 4.7641 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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 (5.96 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 (5.96 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:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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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 2.3820 mL 11.9101 mL 23.8203 mL 59.5507 mL
5 mM 0.4764 mL 2.3820 mL 4.7641 mL 11.9101 mL
10 mM 0.2382 mL 1.1910 mL 2.3820 mL 5.9551 mL
15 mM 0.1588 mL 0.7940 mL 1.5880 mL 3.9700 mL
20 mM 0.1191 mL 0.5955 mL 1.1910 mL 2.9775 mL
25 mM 0.0953 mL 0.4764 mL 0.9528 mL 2.3820 mL
30 mM 0.0794 mL 0.3970 mL 0.7940 mL 1.9850 mL
40 mM 0.0596 mL 0.2978 mL 0.5955 mL 1.4888 mL
50 mM 0.0476 mL 0.2382 mL 0.4764 mL 1.1910 mL
60 mM 0.0397 mL 0.1985 mL 0.3970 mL 0.9925 mL
80 mM 0.0298 mL 0.1489 mL 0.2978 mL 0.7444 mL
100 mM 0.0238 mL 0.1191 mL 0.2382 mL 0.5955 mL
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JNJ-78911118 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-789111183106013-91-3JNJ78911118JNJ 78911118iGluRIonotropic glutamate receptorsGluN2ANAMdepressionrat hippocampal neuronalTBSCFAInhibitorinhibitorinhibit

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