JNJ16259685
Based on 3 publication(s) in Google Scholar
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
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- Pureté: 99.94%
- CAS No.: 409345-29-5
- Formule: C20H23NO3
- Masse moléculaire:325.40
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) JNJ16259685
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Activité biologique
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mGluR1 19 nM (IC50) |
JNJ16259685 potently and completely inhibits the glutamate (30 μM)-induced increase in intracellular Ca2+ concentrations at the rat mGlu1a receptor with an IC50 value of 3.24±1.00 nM. IC50 values for CPCCOEt and BAY 36-7620 are 17.8±10.3 μM and 161±38 nM, respectively. The potency of JNJ16259685 in blocking glutamate (30 μM)-induced Ca2+ mobilization at the human mGlu1a receptor is 1.21±0.53 nM (IC50 n=3). JNJ16259685 inhibits the glutamate (3 μM)-induced rise in intracellular Ca2+ concentrations at the rat mGlu5a receptor with an IC50 value of 1.31±0.39 μM (n=4). JNJ16259685 blocks glutamate (3 μM)-induced Ca2+ mobilization at the human mGlu5 receptor with an IC50 of 28.3±11.7 μM (n=4). JNJ16259685 does not exhibit agonist activity at any of the group I mGlu receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 409345-29-5
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Appearance Solid
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Masse moléculaire 325.40
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Formule C20H23NO3
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Color White to off-white
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SMILES
O=C(C1=CC=C2N=C3C(CCCO3)=CC2=C1)[C@H]4CC[C@@H](OC)CC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Discovery of FO-4-15, a novel 1,2,4-oxadiazole derivative, ameliorates cognitive impairments in 3×Tg mice by activating the mGluR1/CaMKIIα pathway. [Abstract]2025 Jan;46(1):66-80. PMID: 39152295 -
J Transl Med
HuR promotes castration-resistant prostate cancer progression by altering ERK5 activation via posttranscriptional regulation of BCAT1. [Abstract]2024 Feb 18;22(1):178. PMID: 38369471 -
Neurobiol Dis
Impedance-based phenotypic profiling of metabotropic glutamate receptor ligand responses in SCA1 human iPSC-derived neuronal cultures. [Abstract]2026 Mar:220:107296. PMID: 41620186
Solvant et solubilité
DMSO : ≥ 100 mg/mL (307.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (8.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (8.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
Mice[1]
Nine groups of mice are used. Animals are randomLy allocated to two control groups (n=15 each) receiving only saline or saline (90%) plus DMSO (10%), and seven experimental groups (N=14-16 each) receiving JNJ16259685 injections. JNJ16259685 is diluted in saline (90%) plus DMSO (10%) to provide appropriate doses for injections and administered in seven doses: 0.125, 0.25, 0.5, 1, 2, 4 and 8 mg/kg. The doses are chosen on the basis of recent behavioural studies using this compound. Drug or vehicle is injected intraperitoneally in a volume of 10 mL/kg.
Rats[2]
This procedure is used to measure overt behavioral, neurological and autonomic responses to the drug challenge. Briefly, rats are randomLy separated into four groups (n=6), each of which receives a different dose (0, 3, 10, or 30 mg/kg) of JNJ16259685. An expert observer, blind to the drug treatment of the animals, assesses and scores the animals at 30, 60, 120, and 240 min post-injection. The animals are assessed for passivity, body elevation, limb position, limb tone, body tone, gait, and pupil size. For each of these behaviors, a score of 0 is assigned to animals that appeared “normal”, whereas scores of±1,±2, or±3 indicated mild, moderate, or severe increases (+) or decreases (−) from normality. Individual animals that receive a score of±2, or greater, are considered to be significantly effected on the measure. A dose is considered to have a significant effect if 3 or more of the animals receive a score of greater than±2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Navarro JF,et al. JNJ16259685, a selective mGlu1 antagonist, suppresses isolation-induced aggression in male mice. Eur J Pharmacol. 2008 May 31;586(1-3):217-20. [Content Brief]
[2]. Hodgson RA, et al. Characterization of the selective mGluR1 antagonist, JNJ16259685, in rodent models of movement and coordination. Pharmacol Biochem Behav. 2011 Apr;98(2):181-7. [Content Brief]
[3]. Lavreysen H,et al. JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology. 2004 Dec;47(7):961-72. [Content Brief]
[4]. I Fukunaga , et al. Potent and Specific Action of the mGlu1 Antagonists YM-298198 and JNJ16259685 on Synaptic Transmission in Rat Cerebellar Slices. Br J Pharmacol. 2007 Jul;151(6):870-6. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0731 mL | 15.3657 mL | 30.7314 mL | 76.8285 mL |
| 5 mM | 0.6146 mL | 3.0731 mL | 6.1463 mL | 15.3657 mL | |
| 10 mM | 0.3073 mL | 1.5366 mL | 3.0731 mL | 7.6829 mL | |
| 15 mM | 0.2049 mL | 1.0244 mL | 2.0488 mL | 5.1219 mL | |
| 20 mM | 0.1537 mL | 0.7683 mL | 1.5366 mL | 3.8414 mL | |
| 25 mM | 0.1229 mL | 0.6146 mL | 1.2293 mL | 3.0731 mL | |
| 30 mM | 0.1024 mL | 0.5122 mL | 1.0244 mL | 2.5610 mL | |
| 40 mM | 0.0768 mL | 0.3841 mL | 0.7683 mL | 1.9207 mL | |
| 50 mM | 0.0615 mL | 0.3073 mL | 0.6146 mL | 1.5366 mL | |
| 60 mM | 0.0512 mL | 0.2561 mL | 0.5122 mL | 1.2805 mL | |
| 80 mM | 0.0384 mL | 0.1921 mL | 0.3841 mL | 0.9604 mL | |
| 100 mM | 0.0307 mL | 0.1537 mL | 0.3073 mL | 0.7683 mL |
JNJ16259685 Related Classifications
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