JNJ-7777120 459168-41-3

 NJ7777120
分子式：C14H16ClN3O   分子量：277.75
 
產(chǎn)品描述
JNJ-7777120 是*個(gè)，有效的，選擇性非咪唑histamine H4 receptor拮抗劑，Ki為4.5 nM,比作用于其他組胺受體選擇性高1000倍以上。
靶點(diǎn)
Histamine H4 receptor
         
IC50
4.5 nM (Ki)
         
體外研究
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]
體內(nèi)研究
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.
溶解性
DMSO 56 mg/mL，水 <1 mg/mL，乙醇 8 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO