| 產(chǎn)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 |
| 靶點(diǎn)： |
H4 receptor;HistamineReceptor |
| 體內(nèi)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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京