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JNJ-7777120

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Chemical Structure| 459168-41-3 同义名 : -
CAS号 : 459168-41-3
货号 : A568763
分子式 : C14H16ClN3O
纯度 : 98%
分子量 : 277.749
MDL号 : MFCD04343337
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(180.02 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% propylene glycol+5% Tween 80+65% water 20 mg/mL suspension

生物活性
靶点

  • H4 receptor

    Histamine H4 receptor, Ki:4.5 nM
描述 The histamine H4 receptor (H4R) is a completely novel fourth member of the histamine receptor family. There is a fairly selective expression of H4R on bone marrow and hematopoietic cells known to be involved in inflammatory and immune responses [3]. JNJ-7777120 is an effective and selective non-imidazole histamine H4 receptor antagonist with Ki value of 4.5 nM [4]. JNJ-7777120 has an oral bioavailability of approximately 30% in rats and 100% in dogs, with a half-life of approximately 3 h in both species. In mouse bone marrow-derived mast cells, JNJ-7777120 blocks histamine-induced chemotaxis and calcium influx. Furthermore, it can block the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. In a mouse zymosan-induced peritonitis model which is reported to be mast cell-dependent, JNJ-7777120 significantly blocks neutrophil infiltration suggesting that its effect may be mediated by mast cells[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.60mL

0.72mL

0.36mL

18.00mL

3.60mL

1.80mL

36.00mL

7.20mL

3.60mL
参考文献

[1]Rosa AC, Pini A, et al. Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ7777120 treatment. J Pharmacol Exp Ther. 2014 Nov;351(2):308-16.

[2]Jablonowski JA, Grice CA, et al. The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem. 2003 Sep 11;46(19):3957-60.

[3]Thurmond RL. The histamine H4 receptor: from orphan to the clinic. Front Pharmacol. 2015;6:65.

[4]Jablonowski JA, Grice CA, Chai W, et al. The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem. 2003;46(19):3957-3960.

[5]Thurmond RL, Desai PJ, Dunford PJ, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004;309(1):404-413.