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JNJ-7777120
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-7777120图片
CAS NO:459168-41-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)277.75
FormulaC14H16ClN3O
CAS No.459168-41-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 56 mg/mL (201.6 mM)
Water: <1 mg/mL
Ethanol: 8 mg/mL (28.8 mM)
Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 20 mg/mL
SynonymsJNJ7777120; JNJ-7777120; JNJ 7777120
实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits>1000-fold selectivity over the other histamin receptors.


Cell Assay: JNJ-7777120 prevents fibronectin-induced lung fibroblast migration, thus suggesting that H4R could represent an attractive target for the development of new drugs for lung fibrosis treatment .

In VivoJNJ 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.
Animal modelFemale BALB/c mice
Formulation & DosageDissolved in 5% (w/v) dextrose in water; 200 mg/kg; p.o.
ReferencesJ Med Chem. 2003 Sep 11;46(19):3957-60; J Pharmacol Exp Ther. 2004 Apr;309(1):404-13.