JNJ-7777120

Catalog No.S2905 Batch:S290501

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Technical Data

Formula

C14H16ClN3O
Molecular Weight 277.75 CAS No. 459168-41-3
Solubility (25°C)* In vitro DMSO 56 mg/mL (201.62 mM)
Ethanol 8 mg/mL (28.8 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
Targets
Histamine H4 receptor [1]
4.5 nM(Ki)
In vitro JNJ 7777120 binds with high affinity to the H4 receptor and has a greater than 1000-fold selectivity over the other histamine receptors. JNJ 7777120 is a selective and potent H4 receptor antagonist with little or no affinity for over 50 other targets. [2]
In vivo JNJ 7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ∼3 h in both species. JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. JNJ 7777120 can block the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ 7777120 significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. [2]

Protocol (from reference)

Animal Study:[2]
  • Animal Models

    Female BALB/c mice

  • Dosages

    200 mg/kg

  • Administration

    P.O.

Selleck's JNJ-7777120 has been cited by 6 publications

The Host CYP1A1-Microbiota Metabolic Axis Promotes Gut Barrier Disruption in Methicillin-Resistant Staphylococcus aureus-Induced Abdominal Sepsis [ Front Microbiol, 2022, 13:802409] PubMed: 35572636
Effects of Several Therapeutic Agents on Mammalian Vestibular Function: Meclizine, Diazepam, and JNJ7777120 [ J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5] PubMed: 34009490
Anteromedial thalamic nucleus to anterior cingulate cortex inputs modulate histaminergic itch sensation. [ Neuropharmacology, 2020, 168:108028] PubMed: 32151646
P-FN12, an H4R-Based Epitope Vaccine Screened by Phage Display, Regulates the Th1/Th2 Balance in Rat Allergic Rhinitis [ Mol Ther Methods Clin Dev, 2018, 11:83-91] PubMed: 30417023
Histamine Regulates the Inflammatory Profile of SOD1-G93A Microglia and the Histaminergic System Is Dysregulated in Amyotrophic Lateral Sclerosis. [ Front Immunol, 2017, 8:1689] PubMed: 29250069
Evidence for a Role of Orexin/Hypocretin System in Vestibular Lesion-Induced Locomotor Abnormalities in Rats [ Front Neurosci, 2016, 10:355] PubMed: 27507932

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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