| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
JNJ-5207852 is a novel and potent histamine antagonist selective for the H3 subtype. It has stimulant and nootropic effects in animal studies, and has been suggested as a possible treatment for memory defects associated with epilepsy. JNJ-5207852 itself did not progress to clinical development due to poor pharmacokinetic characteristics, but the related compound JNJ-17216498 is currently in Phase II clinical trials for the treatment of narcolepsy.
| ln Vivo |
In H3 receptor knockout mice, JNJ-5207852 (1–10 mg/kg sc) has no effect on wakefulness or sleep, but it enhances wakefulness and decreases REM and slow-wave sleep. H3 receptor antagonists arouse people without the need for strenuous activity. For four weeks, JNJ-5207852 (10 mg/kg ip) administered daily to mice did not cause any changes in body weight. After oral treatment, JNJ-5207852 is well absorbed and reaches high brain levels [1].
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| Animal Protocol |
Animal/Disease Models: Male, SD (SD (Sprague-Dawley)) rat, weight 282-334 grams [1].
Doses: 3, 10, 30 mg/kg. Route of Administration: SC Experimental Results: Increased wakefulness and diminished REM and slow wave sleep. |
| References |
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| Molecular Formula |
C20H32N2O
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|---|---|
| Molecular Weight |
316.48088
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| Exact Mass |
316.251
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| CAS # |
398473-34-2
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| Related CAS # |
JNJ-5207852 dihydrochloride;1782228-76-5
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
443.4±30.0 °C at 760 mmHg
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| Flash Point |
123.9±21.8 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.542
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| LogP |
4.11
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| InChi Key |
PTKHFRNHJULJKT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H32N2O/c1-3-12-21(13-4-1)16-7-17-23-20-10-8-19(9-11-20)18-22-14-5-2-6-15-22/h8-11H,1-7,12-18H2
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| Chemical Name |
1-{3-[4-(Piperidin-1-ylmethyl)phenoxy]propyl}piperidine
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| Synonyms |
JNJ-5207852; JNJ5207852; JNJ 5207852
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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 : ~77.5 mg/mL (~244.88 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.58 mg/mL (8.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.8 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: ≥ 2.58 mg/mL (8.15 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 25.8 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. View More
Solubility in Formulation 3: ≥ 2.58 mg/mL (8.15 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 | 3.1598 mL | 15.7988 mL | 31.5976 mL | |
| 5 mM | 0.6320 mL | 3.1598 mL | 6.3195 mL | |
| 10 mM | 0.3160 mL | 1.5799 mL | 3.1598 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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