JNJ-7777120

Catalog No.S2905

For research use only.

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.

JNJ-7777120 Chemical Structure

CAS No. 459168-41-3

Selleck's JNJ-7777120 has been cited by 5 Publications

Purity & Quality Control

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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 Research:[2]
  • Animal Models: Female BALB/c mice
  • Dosages: 200 mg/kg
  • Administration: P.O.
  • (Only for Reference)

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
(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.

20 mg/mL

* 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.

Chemical Information

Molecular Weight 277.75
Formula

C14H16ClN3O

CAS No. 459168-41-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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