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Purity: ≥98%
JNJ-42153605 is a potent, selective and allosteric modulator of the mGlu2 (metabotropic glutamate 2) receptor with with an EC50 of 17 nM. It exhibits a superior pharmacokinetic profile in both rodent and nonrodent variants. It is determined that JNJ-42153605 is not an agonist or antagonist toward other mGlu receptor subtypes up to 30 μM when its selectivity for the mGlu2 receptor is evaluated. With no signs of P-glycoprotein efflux, JNJ-42153605 exhibits high permeability. Using a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, JNJ-42153605 demonstrated a central in vivo efficacy by inhibiting the REM sleep state, a phenomenon previously demonstrated to be mGlu2 mediated. Using an ED₩₀ of 5.4 mg/kg sc, which is suggestive of antipsychotic activity, JNJ-42153605 reversed PCP-induced hyperlocomotionin mice.
| Targets |
mGluR2 ( EC50 = 17 nM )
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| References |
| Molecular Formula |
C₂₂H₂₃F₃N₄
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| Molecular Weight |
400.44
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| Exact Mass |
400.19
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| Elemental Analysis |
C, 65.99; H, 5.79; F, 14.23; N, 13.99
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| CAS # |
1254977-87-1
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| Appearance |
Solid powder
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| SMILES |
C1CC1CC2=NN=C3N2C=CC(=C3C(F)(F)F)N4CCC(CC4)C5=CC=CC=C5
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| InChi Key |
BQAVZGJJQFJSMW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23F3N4/c23-22(24,25)20-18(10-13-29-19(14-15-6-7-15)26-27-21(20)29)28-11-8-17(9-12-28)16-4-2-1-3-5-16/h1-5,10,13,15,17H,6-9,11-12,14H2
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| Chemical Name |
3-(cyclopropylmethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (4.17 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (4.17 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 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4973 mL | 12.4863 mL | 24.9725 mL | |
| 5 mM | 0.4995 mL | 2.4973 mL | 4.9945 mL | |
| 10 mM | 0.2497 mL | 1.2486 mL | 2.4973 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.
J Med Chem.2012 Oct 25;55(20):8770-89. |
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