Home Neuronal Signaling Histamine Receptor antagonist JNJ-7777120 For research use only.

JNJ-7777120

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

JNJ-7777120 Chemical Structure

CAS: 459168-41-3

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

Purity & Quality Control

Batch: S290501 DMSO] 56 mg/mL] false] Ethanol] 8 mg/mL] false] Water] Insoluble] false Purity: 99.97%
99.97

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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
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
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]
Animal Research Animal Models Female BALB/c mice
Dosages 200 mg/kg
Administration P.O.

Chemical lnformation & Solubility

Molecular Weight 277.75 Formula

C14H16ClN3O
CAS No. 459168-41-3 SDF Download JNJ-7777120 SDF
Smiles CN1CCN(CC1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 56 mg/mL ( (201.62 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


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In vivo
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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.

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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.

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