| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
OX2 receptor (OX2R).
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|---|---|
| ln Vitro |
JNJ-10397049 is a selective OX2R antagonist with a pIC50 of 7.4 for chimeric OX2 receptors, a pKi of 8.3, and pKB values of 5.9 and 8.5 for OX1 and OX2 receptors, respectively. It exhibits >600-fold selectivity for OX2R over OX1R. In a panel of more than 50 other neurotransmitter and neuropeptide receptors, it exhibits no discernible activity.
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| ln Vivo |
JNJ-10397049 (10–30 mg/kg) lengthens the duration of nonrapid and rapid eye movement sleep and reduces the latency for persistent sleep[2].
JNJ-10397049 inhibits reinstatement, place preference, and self-administration of ethanol[3]. In rats, JNJ-10397049 produces a high level of OX2 receptor occupancy in the brain. When administered subcutaneously to rats at 10-30 mg/kg, it promotes sleep by lengthening the duration of non-rapid and rapid eye movement sleep and reducing the latency to persistent sleep. It also inhibits reinstatement, place preference, and self-administration of ethanol. |
| Enzyme Assay |
Radioligand binding assays using membrane preparations from cells expressing recombinant OX1 or OX2 receptors, incubated with the compound and a labeled orexin peptide (e.g., [125I]orexin-A), to determine receptor binding affinity (Ki or pKi). The assay typically involves incubation at room temperature, followed by filtration and scintillation counting.
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| Cell Assay |
Functional assays (e.g., calcium mobilization or IP accumulation) in cells expressing OX2 receptors to evaluate antagonist potency (pIC50 or pKB). Cells are preincubated with the compound and then stimulated with orexin-A, and the receptor-mediated response is measured to determine the compound's ability to block orexin signaling.
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| Animal Protocol |
Male Sprague-Dawley rats
10 mg/kg Subcutaneous administration. Male Sprague-Dawley rats administered compound subcutaneously at 10-30 mg/kg; sleep-wake architecture monitored by electroencephalography/electromyography (EEG/EMG) to assess effects on sleep duration, latency, and architecture. Functional magnetic resonance imaging (fMRI) is used to assess the compound's effects on brain activity. |
| References |
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| Molecular Formula |
C19H20BR2N2O3
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|---|---|---|
| Molecular Weight |
484.18
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| Exact Mass |
481.984
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| Elemental Analysis |
C, 47.13; H, 4.16; Br, 33.01; N, 5.79; O, 9.91
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| CAS # |
708275-58-5
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| Related CAS # |
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| PubChem CID |
9869934
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
521.1±50.0 °C at 760 mmHg
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| Flash Point |
268.9±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.647
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| LogP |
5.66
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
485
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1(OC[C@H](NC(NC2=C(Br)C=C(Br)C=C2)=O)[C@@H](O1)C3=CC=CC=C3)C
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| InChi Key |
RBKIJGLHFFQHBE-IRXDYDNUSA-N
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| InChi Code |
InChI=1S/C19H20Br2N2O3/c1-19(2)25-11-16(17(26-19)12-6-4-3-5-7-12)23-18(24)22-15-9-8-13(20)10-14(15)21/h3-10,16-17H,11H2,1-2H3,(H2,22,23,24)/t16-,17-/m0/s1
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| Chemical Name |
1-(2,4-dibromophenyl)-3-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]urea
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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: 4.25 mg/mL (8.78 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 42.5 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: ≥ 4.25 mg/mL (8.78 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 42.5 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 | 2.0653 mL | 10.3267 mL | 20.6535 mL | |
| 5 mM | 0.4131 mL | 2.0653 mL | 4.1307 mL | |
| 10 mM | 0.2065 mL | 1.0327 mL | 2.0653 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.
fMRI activation produced by D-amphetamine as a function of pharmacological pre-treatment.PLoS One.2011 Jan 28;6(1):e16406. |
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 fMRI timecourse in representative brain regions: effect of OX2R antagonism.PLoS One.2011 Jan 28;6(1):e16406. |
Attenuation of fMRI response by OX1R or OX2R antagonism. Regions of reduced amphetamine-induced rCBV response following pre-treatment with GSK1059865 (OX1Rant; top) or JNJ10397049 (OX2Rant, bottom). Blue indicatesreducedrCBV response versus control (vehicle-amphetamine). Cpu: caudate putamen; SS ctx: somatosensory cortex; Ins: insular cortex, AcS: shell of the nucleus accumbens. |
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