JNJ-7777120

Research use only, not for human use.

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.

JNJ7777120 is a potent and selective histamine H4 receptor antagonist. JNJ7777120 induces increases in the histamine content of the rat conjunctiva. In vivo studies showed that JNJ7777120 significantly suppressed nasal symptoms and the number of coughs. JNJ7777120 significantly inhibited airway reactivity to histamine.

Cell Viability Assay Cell Line:SK-N-MC cells (expressing the human or mouse histamine H4 receptor)Concentration:0, 10, 100, 1000 nM Incubation Time:~6 h Result:Exhibited antagonistic effect on human and mouse histamine H4 receptors.Immunofluorescence Cell Line:Mouse mast cells Concentration:10 μM Incubation Time:10 min Result:Exhibited a very potent antagonistic effect on the H4 receptor in primary cells.Cell Viability Assay Cell Line:BMMC Concentration:30-100 μM Incubation Time:30 min Result:Significantly inhibited the production of TARC (thymus and activation-regulated chemokine) and MDC (macrophage-derived chemokine).

Animal Model:BALB/c mice.Dosage:20 mg/kg Administration:Subcutaneous injection; single daily for 2 days Result:Blocked histamine induced an increase in the number of mast cells per tracheal section and a significant migration of mast cells towards the tracheal epithelium.Animal Model:Male outbred Swiss albino mice (zymosan-induced peritonitis model).Dosage:10 mg/kg Administration:Subcutaneous injection; single Result:Led to a statistically significant reduction of neutrophil infiltration.

JNJ7777120 | JNJ-7777120

Immunology/Inflammation

LTR

H4 receptor

Inflammation/Immunology

——

459168-41-3

277.75

C14H16ClN3O

>98% (HPLC)

DMSO : ≥ 50 mg/mL; 180.02 mM

CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl

1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine

(-20℃)

With Ice Pack

≥ 2 years