| CAS NO: | 459168-41-3 |
| 规格: | ≥98% |
| 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 |
| Molecular Weight (MW) | 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 | JNJ7777120; JNJ-7777120; JNJ 7777120 |
| 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 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. |
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