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  4. JNJ-55511118

JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a Ki of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures.

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JNJ-55511118

JNJ-55511118 Chemical Structure

CAS No. : 2036081-86-2

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Description

JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a Ki of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures[1][2].

IC50 & Target[2]

AMPA Receptor

26 nM (Ki)

In Vitro

JNJ-55511118 is a potent, selective negative modulator of TARP-γ8-containing AMPA receptors, with a mean pIC50 value ranging from 7.42 to 8.33 across human, rat, mouse, monkey, and canine GluA-γ8 combinations, and it shows no activity against TARP-containing AMPA receptors without γ8 or TARP-free AMPA receptors[2].
JNJ-55511118 (1 μM; 50-60 s) partially inhibits glutamate-evoked currents in heterologously expressed TARP-γ8-containing AMPA receptors by accelerating desensitization and inactivation processes[2].
JNJ-55511118 exerts weak antagonistic activity against human 5-HT2B receptors (IC50 = 6 μM)[2].

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

JNJ-55511118 Related Antibodies
In Vivo

JNJ-55511118 (0-10 mg/kg; p.o.; single administration) significantly reduces multiple indices of voluntary sweet wine intake in male C57BL/6J mice, without decreasing parameters related to voluntary sweet wine consumption in female C57BL/6J mice, but the 10 mg/kg dose alters lever discrimination behavior by increasing the number of responses on the inactive lever[1].
JNJ-55511118 (i.v./p.o., 0-10 mg/kg, single administration) dose-dependently suppresses population spikes in the hippocampal CA1 region in anesthetized rats, with an ED50 of 0.4 mg/kg for intravenous injection. It also dose-dependently reduces cortical electroencephalogram power across multiple frequency bands in freely moving rats, and transient hyperactivity occurs at the oral dose of 10 mg/kg[2].
JNJ-55511118 (p.o.; single dose, 0-40 mg/kg) exerts potent, near-complete seizure protection in corneal and amygdala-kindled mouse models, with an oral ED50 of 3.7 mg/kg. It produces partially dose-dependent seizure protection in the 6 Hz psychomotor seizure model of *Mus musculus*, with ED50 values of 18.3 mg/kg p.o. (32 mA) and 6.5 mg/kg p.o. (44 mA), respectively, and elevates the convulsive threshold of mice to PTZ[2].

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

Animal Model: C57BL/6J (male/female)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Reduced alcohol-reinforced response rate from 10 to 60 minutes post-administration compared to vehicle.
Reduced total active lever presses, number of alcohol reinforcers earned, and alcohol intake (g/kg/1h) compared to vehicle.
Decreased percentage of responses on the active lever from 92.4 (vehicle) to 76.5 ± 5 (1 mg/kg) and 75.7 (10 mg/kg).
Increased inactive lever responding at 10 mg/kg dose.
Showed no effect on open-field ambulatory distance in alcohol-exposed or sucrose-exposed mice at 1 mg/kg dose.
Showed no effect on sucrose-only self-administration parameters.
Showed no effect on alcohol-reinforced response rate, total active lever presses, number of alcohol reinforcers earned, or alcohol intake (g/kg/1h).
Reduced percentage of responses on the active lever from 92 (vehicle) to 79.9 at 10 mg/kg dose.
Increased inactive lever responding at 10 mg/kg dose.
Showed no effect on sucrose-only self-administration parameters.
Animal Model: Sprague-Dawley (male, 300-450 grams)[2]
Dosage: 0, 0.25, 0.5, 1, 2, 3, 4, 8, 10 mg/kg
Administration: i.v./p.o., single dose
Result: Caused rapid, dose-dependent inhibition of evoked population spike amplitude.
Fitted an ED50 of 0.4 mg/kg i.v.
for inhibition.
Achieved near-complete inhibition of population spikes at 8 mg/kg.
Reached an EC50 of 591 ng/mL for population spike inhibition based on brain concentration, which closely matched the EC50 for target occupancy (545 ng/mL).
Caused dose-dependent decrease in wake-state EEG power across theta (4-10 Hz), alpha (10-15 Hz), and beta (15-30 Hz) bands; at 10 mg/kg, power was reduced to 81.2%, 70.6%, and 63.8% of vehicle control, respectively.
Induced a small, significant decrease in delta (1-4 Hz) power only at 1 mg/kg.
Caused significant, transient increase in locomotor activity for approximately 1 hour post-dose at 10 mg/kg.
Induced dose-dependent increase in latency to REM and NREM sleep.
Caused dose-dependent decreases in absolute EEG power during NREM and REM sleep.
Animal Model: albino CF1 (male)[2]
Dosage: 0-40 mg/kg
Administration: p.o.; single dose
Result: Provided near-complete seizure protection at doses ≥5 mg/kg p.o.: 25/32 animals at these doses had Racine scores of 0, compared to 0/8 vehicle-treated animals.
Fitted an ED50 of 3.7 mg/kg p.o.
for seizure protection, with an EC50 of 938 ng/mL based on brain concentration.
Provided partial seizure protection: at doses ≥10 mg/kg p.o., 12/32 animals were protected in the 32 mA model, and 11/40 animals were protected in the 44 mA model.
Fitted an ED50 of 18.3 mg/kg p.o.
for the 32 mA model (76% maximum protection, EC50 4644 ng/mL plasma concentration) and 6.5 mg/kg p.o.
for the 44 mA model (22% maximum protection, EC50 2533 ng/mL plasma concentration).
Significantly increased the PTZ threshold for clonus from 33.3 mg/kg to 49.5 mg/kg.
Significantly increased the PTZ threshold for twitch from 30.7 g/kg to 42.4 mg/kg.
Protected 11/12 rats from seizure, compared to 1/12 rats protected with vehicle.
Significantly reduced mean afterdischarge duration from 92 seconds (vehicle) to 35 seconds.
Molecular Weight

328.67

Formula

C14H8ClF3N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=C(N1)C=C(C3=C(OC(F)(F)F)C=CC=C3Cl)C=C2
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 (304.26 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0426 mL 15.2128 mL 30.4257 mL
5 mM 0.6085 mL 3.0426 mL 6.0851 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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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 (7.61 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 (7.61 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 3.0426 mL 15.2128 mL 30.4257 mL 76.0641 mL
5 mM 0.6085 mL 3.0426 mL 6.0851 mL 15.2128 mL
10 mM 0.3043 mL 1.5213 mL 3.0426 mL 7.6064 mL
15 mM 0.2028 mL 1.0142 mL 2.0284 mL 5.0709 mL
20 mM 0.1521 mL 0.7606 mL 1.5213 mL 3.8032 mL
25 mM 0.1217 mL 0.6085 mL 1.2170 mL 3.0426 mL
30 mM 0.1014 mL 0.5071 mL 1.0142 mL 2.5355 mL
40 mM 0.0761 mL 0.3803 mL 0.7606 mL 1.9016 mL
50 mM 0.0609 mL 0.3043 mL 0.6085 mL 1.5213 mL
60 mM 0.0507 mL 0.2535 mL 0.5071 mL 1.2677 mL
80 mM 0.0380 mL 0.1902 mL 0.3803 mL 0.9508 mL
100 mM 0.0304 mL 0.1521 mL 0.3043 mL 0.7606 mL
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  • 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-555111182036081-86-2JNJ55511118JNJ 55511118iGluRIonotropic glutamate receptorsAMPA receptor Modulatoralcohol use disorderseizuresalbino CF1 miceSprague-Dawley ratC57BL/6J miceInhibitorinhibitorinhibit

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