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JNJ-7777120 {[allProObj[0].p_purity_real_show]}

货号:A568763

JNJ-7777120 is a selective antagonist of histamine-4 receptor (H4R) with Ki of 4 ± 1 nM.

JNJ-7777120 化学结构 CAS号:459168-41-3
JNJ-7777120 化学结构
CAS号:459168-41-3
JNJ-7777120 3D分子结构
CAS号:459168-41-3
JNJ-7777120 化学结构 CAS号:459168-41-3
JNJ-7777120 3D分子结构 CAS号:459168-41-3
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JNJ-7777120 纯度/质量文件 产品仅供科研

货号:A568763 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 99%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

JNJ-7777120 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].

JNJ-7777120 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.

JNJ-7777120 实验方案

计算器
存储液制备 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

JNJ-7777120 技术信息

CAS号459168-41-3
分子式C14H16ClN3O
分子量 277.749
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

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

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