JNJ-46281222
Based on 1 Customer Validation
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
For research use only. We do not sell to patients.
- Purity: 98.77%
- CAS No.: 1254980-38-5
- Formula: C23H25F3N4
- Molecular Weight:414.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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mGluR2 1.7 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
21 nM
Compound: 12
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Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method
Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method
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[PMID: 27579727] |
JNJ-4628122 binds to the selected mGlu2 receptor mutants is significantly decreased by approximately 10-fold compared with WT, in transfected mGlu2 WT and mutant receptors in CHO-K1 cells, mutations F643A and N735D are selected[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO‐K1 cells
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Concentration:
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Incubation Time:
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Result:Showed a decreased expression of mGlu2 receptor in mutant cells.
Chemical Information
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CAS No. 1254980-38-5
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Appearance Solid
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Molecular Weight 414.47
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Formula C23H25F3N4
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Color White to off-white
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SMILES
FC(C1=C(CN2CCC(C3=CC=CC=C3)CC2)C=CN4C1=NN=C4CC5CC5)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 62.5 mg/mL (150.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 |
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| DMSO | 1 mM | 2.4127 mL | 12.0636 mL | 24.1272 mL | 60.3180 mL |
| 5 mM | 0.4825 mL | 2.4127 mL | 4.8254 mL | 12.0636 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4127 mL | 6.0318 mL | |
| 15 mM | 0.1608 mL | 0.8042 mL | 1.6085 mL | 4.0212 mL | |
| 20 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0159 mL | |
| 25 mM | 0.0965 mL | 0.4825 mL | 0.9651 mL | 2.4127 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8042 mL | 2.0106 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5079 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL | 1.2064 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4021 mL | 1.0053 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7540 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2413 mL | 0.6032 mL |
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