产品描述: JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory |
靶点:
H4 receptor;HistamineReceptor |
体内研究:
JNJ-7777120 shows equipotent against the human, mouse, and rat receptors and exhibits at least 1000-fold selectivity over H1, H2, or H3 receptors. 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 (20 mg/kg; s.c.; single daily for 2 days) blocks the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ-7777120 (10 mg/kg; s.c.; single) significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. 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. |
参考文献:
1. Thurmond RL, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004 Apr;309(1):404-13. 2. Ohsawa Y, et al. The antagonism of histamine H1 and H4 receptors ameliorates chronic allergic dermatitis via anti-pruritic and anti-inflammatory effects in NC/Nga mice. Allergy. 2012 Aug;67(8):1014-22. |
溶解性:
Soluble in DMSO |
保存条件:
2-8℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
3.6 ml |
18.002 ml |
36.004 ml |
5 mM |
0.72 ml |
3.6 ml |
7.201 ml |
10 mM |
0.36 ml |
1.8 ml |
3.6 ml |
50 mM |
0.072 ml |
0.36 ml |
0.72 ml |
|
注意: |
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