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JNJ-46281222 is a novel, selective, and highly potent positive allosteric modulator of the mGlu2 (metabotropic glutamate) receptor. It has nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
| ln Vitro |
When mGlu2 WT and CHO-K1 cells were transfected, the mGlu2 receptor mutants F643A and N735D were chosen for the mutant receptor, and binding of JNJ-4628122 to these mutants was dramatically reduced, around ten times less than in WT [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: CHO-K1 Cell Tested Concentrations: Incubation Duration: Experimental Results: The expression of mGlu2 receptor was diminished in mutant cells. |
| References |
| Molecular Formula |
C23H25F3N4
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|---|---|
| Molecular Weight |
414.466615438461
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| Exact Mass |
414.203
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| CAS # |
1254980-38-5
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| Related CAS # |
1254980-38-5
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| PubChem CID |
49822115
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
567
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(F)(F)C1C2=NN=C(CC3CC3)N2C=CC=1CN1CCC(C2C=CC=CC=2)CC1
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| InChi Key |
LYDKDODJIBQNLK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25F3N4/c24-23(25,26)21-19(10-13-30-20(14-16-6-7-16)27-28-22(21)30)15-29-11-8-18(9-12-29)17-4-2-1-3-5-17/h1-5,10,13,16,18H,6-9,11-12,14-15H2
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| Chemical Name |
3-(cyclopropylmethyl)-7-[(4-phenylpiperidin-1-yl)methyl]-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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| Synonyms |
JNJ-46281222 JNJ 46281222 JNJ46281222.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~150.79 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4127 mL | 12.0636 mL | 24.1272 mL | |
| 5 mM | 0.4825 mL | 2.4127 mL | 4.8254 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4127 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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