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

货号:A568763 Ambeed 开学季,买赠积分,赢豪礼

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 {[allProObj[0].p_purity_real_show]}
Cyclizine {[allProObj[0].p_purity_real_show]}
Loratadine +

B(0)AT2, IC50: 4 μM

{[allProObj[0].p_purity_real_show]}
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

{[allProObj[0].p_purity_real_show]}
Doxylamine succinate {[allProObj[0].p_purity_real_show]}
Ebastine {[allProObj[0].p_purity_real_show]}
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

{[allProObj[0].p_purity_real_show]}
Meclizine dihydrochloride {[allProObj[0].p_purity_real_show]}
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

{[allProObj[0].p_purity_real_show]}
Diphenhydramine HCl {[allProObj[0].p_purity_real_show]}
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

{[allProObj[0].p_purity_real_show]}
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

{[allProObj[0].p_purity_real_show]}
Bilastine +++

H1 receptor, Ki: 44.15 nM

{[allProObj[0].p_purity_real_show]}
Pemirolast potassium {[allProObj[0].p_purity_real_show]}
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

{[allProObj[0].p_purity_real_show]}
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

{[allProObj[0].p_purity_real_show]}
Brompheniramine maleate {[allProObj[0].p_purity_real_show]}
Carbinoxamine maleate salt {[allProObj[0].p_purity_real_show]}
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

{[allProObj[0].p_purity_real_show]}
Ketotifen fumarate salt {[allProObj[0].p_purity_real_show]}
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR {[allProObj[0].p_purity_real_show]}
Famotidine {[allProObj[0].p_purity_real_show]}
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

{[allProObj[0].p_purity_real_show]}
Lafutidine {[allProObj[0].p_purity_real_show]}
Cimetidine {[allProObj[0].p_purity_real_show]}
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE {[allProObj[0].p_purity_real_show]}
Ranitidine {[allProObj[0].p_purity_real_show]}
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

{[allProObj[0].p_purity_real_show]}
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

{[allProObj[0].p_purity_real_show]}
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

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

Histamine H4 receptor, Ki: 4.5 nM

{[allProObj[0].p_purity_real_show]}
Azelastine HCl {[allProObj[0].p_purity_real_show]}
Epinastine HCl {[allProObj[0].p_purity_real_show]}
Levodropropizine {[allProObj[0].p_purity_real_show]}
Cyproheptadine hydrochloride {[allProObj[0].p_purity_real_show]}
Hesperetin {[allProObj[0].p_purity_real_show]}
Olopatadine HCl {[allProObj[0].p_purity_real_show]}
Mianserin hydrochloride {[allProObj[0].p_purity_real_show]}
Buclizine 2HCl {[allProObj[0].p_purity_real_show]}
Latrepirdine 2HCl GluR {[allProObj[0].p_purity_real_show]}
Cetirizine 2HCl {[allProObj[0].p_purity_real_show]}
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

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

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