product name JNJ-7777120
Description: JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM. 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.
References: J Med Chem. 2003 Sep 11;46(19):3957-60; J Pharmacol Exp Ther. 2004 Apr;309(1):404-13.
277.75
Formula
C14H16ClN3O
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
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427851
| 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: Cell Assay: |
|---|---|
| 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. |
| Animal model | Female BALB/c mice |
| Formulation & Dosage | Dissolved in 5% (w/v) dextrose in water; 200 mg/kg; p.o. |
| References | J Med Chem. 2003 Sep 11;46(19):3957-60; J Pharmacol Exp Ther. 2004 Apr;309(1):404-13. |
