JNJ-7777120
目录号 : GC10400
JNJ-7777120是一种组胺H4受体（H4R：Ki = 4.5nM）拮抗剂。
Cas No.:459168-41-3
Sample solution is provided at 25 µL, 10mM.
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JNJ-7777120 is a histamine H4 receptor (H4R: Ki = 4.5nM) antagonist [1]. JNJ-7777120 can inhibit the production of CCL17 and CCL22 by marrow-derived mast cells (BMMCs) under antigen stimulation, thereby reducing the inflammatory response and improving dermatitis symptoms [2]. JNJ-7777120 is primarily used to relieve inflammation and brain damage [3].
In human peripheral blood neutrophils, JNJ-7777120 (0.001, 0.01, 0.1, 1, 10μM; 30 minutes) can specifically antagonize H4 receptors and restore the degranulation function of neutrophils, verifying that H4 receptors play a negative regulatory role in inhibiting the inflammatory process [4]. In Th17 cells, the trend of cellular IL-17 secretion was inhibited after adding JNJ-7777120 (10μM; 1h) [5].
In mild traumatic brain injury (mTBI) rat model, JNJ-7777120 (1mg/kg; ip; twice/day for 7 days) treatments markedly attenuate the impairment in motor-sensory-reflex and balance functions caused by mild TBI in rats [6]. In a mouse allergic asthma model, JNJ-7777120 (20mg/kg; sc; single injection) can alleviate asthma symptoms [7]. In the LPS mouse model, JNJ-7777120 (5, 10, 20mg/kg; po; single dose) treatment reduced TNF levels [8].
References:
[1]. Thurmond RL, Desai PJ, Dunford PJ, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. The Journal of pharmacology and experimental therapeutics. 2004 Apr 1; 309(1): 404-413.
[2]. Ohsawa Y, Hirasawa N. The antagonism of histamine H 1 and H 4 receptors ameliorates chronic allergic dermatitis via anti‐pruritic and anti‐inflammatory effects in NC/N ga mice. Allergy. 2012 Aug; 67(8): 1014-1022.
[3]. Correa MF, dos Santos Fernandes JP. Targeting the Histamine H4 Receptor: Future Drugs for Inflammatory Diseases. Current Organic Chemistry. 2018 Jul 1; 22(17): 1663-1672.
[4]. Dib K, Perecko T, Jenei V, et al. The histamine H4 receptor is a potent inhibitor of adhesion-dependent degranulation in human neutrophils. Journal of Leukocyte Biology. 2014 Sep; 96(3): 411-418.
[5]. Han SH, Hur MS, Kim MJ, et al. Preliminary study of histamine H4 receptor expressed on human CD4+ T cells and its immunomodulatory potency in the IL-17 pathway of psoriasis. Journal of dermatological science. 2017 Oct 1; 88(1): 29-35.
[6]. Saglam-Cifci E, Gulec I, Sengelen A, et al. The H4R antagonist, JNJ-7777120 treatments ameliorate mild traumatic brain injury by reducing oxidative damage, inflammatory and apoptotic responses through blockage of the ERK1/2/NF-kB pathway in a rat model. Experimental Neurology. 2025 Mar 1; 385: 115133.
[7]. Beermann S, Glage S, Jonigk D, et al. Opposite effects of mepyramine on JNJ 7777120-induced amelioration of experimentally induced asthma in mice in sensitization and provocation. PloS one. 2012 Jan 17; 7(1): e30285.
[8]. Cowden JM, Yu F, Challapalli M, et al. Antagonism of the histamine H 4 receptor reduces LPS-induced TNF production in vivo. Inflammation Research. 2013 Jun; 62: 599-607.
JNJ-7777120是一种组胺H4受体（H4R：Ki = 4.5nM）拮抗剂 [1]。JNJ-7777120可以抑制骨髓来源的肥大细胞（BMMC）在抗原刺激下产生CCL17和CCL22，从而减轻炎症反应并改善皮炎症状 [2]。JNJ-7777120 主要用于缓解炎症和脑损伤 [3]。
在人外周血中性粒细胞中，JNJ-7777120（0.001、0.01、0.1、1、10μM；30分钟）可特异性拮抗H4受体，恢复中性粒细胞的脱颗粒功能，验证了H4受体在抑制炎症过程中起负调控作用 [4]。在Th17细胞中，添加JNJ-7777120（10μM；1h）后，细胞IL-17分泌趋势受到抑制 [5]。
在轻度创伤性脑损伤（mTBI）大鼠模型中，JNJ-7777120（1mg/kg；ip；每日两次，共7天）治疗显著减轻了轻度TBI对大鼠运动感觉反射和平衡功能的损害 [6]。在小鼠过敏性哮喘模型中，JNJ-7777120（20mg/kg；sc；单次注射）可以缓解哮喘症状 [7]。在LPS小鼠模型中，JNJ-7777120（5、10、20mg/kg；po；单次给药）治疗降低了TNF水平 [8]。
| Cell experiment [1]: | |
Cell lines | Human peripheral blood neutrophils (PMNs) |
Preparation Method | JNJ-7777120 was used as a selective histamine H4 receptor antagonist in in vitro experiments with PMNs. Cells were pre-incubated with JNJ-7777120 for 5 minutes at 37°C prior to stimulation with fMLP (0.1μM) on fibrinogen-coated plates to induce Mac-1 dependent degranulation. Lactoferrin release was quantified after 30 minutes as a readout of granule secretion. |
Reaction Conditions | 0.001, 0.01, 0.1, 1, 10μM; 30 minutes |
Applications | JNJ-7777120 reversed the inhibitory effect of histamine on degranulation in a dose-dependent manner, with complete restoration observed at 1μM and an IC₅₀ of approximately 0.05μM. |
| Animal experiment [2]: | |
Animal models | Mild traumatic brain injury (mTBI) rat model |
Preparation Method | JNJ-7777120 was dissolved in DMSO and then diluted in 0.9 % isotonic sodium chloride. Intraperitoneal injection of JNJ-7777120 (1mg/kg) was initiated one hour after TBI and continued twice daily (the interval between two injections was 12h) for one-week. |
Dosage form | 1mg/kg; ip; twice/day for 7 days |
Applications | JNJ-7777120 treatments markedly attenuate the impairment in motor-sensory-reflex and balance functions caused by mild TBI in rats. |
References: | |
| Cas No. | 459168-41-3 | SDF | |
| 化学名 | (5-chloro-1H-indol-2-yl)-(4-methylpiperazin-1-yl)methanone | ||
| Canonical SMILES | CN1CCN(CC1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl | ||
| 分子式 | C14H16ClN3O | 分子量 | 277.75 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 14 mg/ml,Ethanol: 2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6004 mL | 18.0018 mL | 36.0036 mL |
| 5 mM | 0.7201 mL | 3.6004 mL | 7.2007 mL |
| 10 mM | 0.36 mL | 1.8002 mL | 3.6004 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet