JNJ-7777120 |
カタログ番号GC10400
One-Click Copy Product Info
|
JNJ-7777120はヒスタミンH4受容体(H4R: Ki = 4.5nM)拮抗剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 459168-41-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
JNJ-7777120はヒスタミンH4受容体(H4R: Ki = 4.5nM)拮抗剤である[1]。JNJ-7777120は、骨髄由来の肥満細胞(BMMCs)が抗原刺激の下でのCCL17とCCL22の産生を阻害でき、よって炎症反応を減らし、皮膚炎の症状を改善する[2]。JNJ-7777120は主に、炎症と脳損傷の緩和に使われる[3]。
ヒト末梢血好中球で、JNJ-7777120 (0.001, 0.01, 0.1, 1, 10μM；30分間)は特異的にH4受容体を拮抗し、好中球の脱顆粒機能を回復させ、H4受容体が炎症プロセスの阻害で負の規制的役割を果たしていることを検証する[4]。Th17細胞で、JNJ-7777120 (10μM；1時間)の添加後、細胞IL-17分泌の傾向は阻害された[5]。
軽度外傷性脳損傷(mTBI)ラットモデルで、JNJ-7777120 (1mg/kg；腹腔内；2回/日、7日間)の処理は、ラットで、軽度TBIによる運動感覚反射とバランス機能の損傷を著しく軽減した[6]。ラットアレルギー喘息モデルで、JNJ-7777120 (20mg/kg；皮下；単回注射)は喘息の症状を軽減できる[7]。LPSマウスモデルで、JNJ-7777120 (5, 10, 20mg/kg；経口；単回投与)の処理は、TNFレベルを減らした[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.
| 細胞実験[1]: | |
細胞株 | ヒト末梢血好中球(PMNs) |
準備方法 | JNJ-7777120は、PMNsとの体外実験で、選択的なヒスタミンH4受容体の拮抗剤として使われた。細胞を37℃で、JNJ-7777120と共に5分間事前培養し、その後は、フィブリノーゲンでコーティングされたプレートで、fMLP (0.1μM)で刺激し、よってMac-1依存の脱顆粒を誘発した。Lactoferrinの放出を、顆粒分泌の読取り値として30分後に定量した。 |
反応条件 | 0.001, 0.01, 0.1, 1, 10μM；30分間 |
アプリケーション | JNJ-7777120は脱顆粒におけるヒスタミンの阻害効果を用量依存的に逆転させ、1μMで完全な回復が観察され、IC₅₀は約0.05μMであった。 |
| 動物実験 [2]: | |
動物モデル | 軽度外傷性脳損傷(mTBI)ラットモデル |
準備方法 | JNJ-7777120をDMSOに溶解し、0.9%の等張塩化ナトリウムで希釈した。TBIの1時間後に、JNJ-7777120(1mg/kg)の腹腔内注射を開始し、1週間で、毎日二回投与した（間隔は12時間）。 |
投与形態 | 1mg/kg；腹腔内；2回/日、7日間 |
アプリケーション | JNJ-7777120の処理は、軽度TBIによる運動感覚反射とバランス機能の損傷を著しく軽減した。 |
References: | |
| Cas No. | 459168-41-3 | SDF | |
| Chemical Name | (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 | ||
| Formula | C14H16ClN3O | M.Wt | 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 | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6004 mL | 18.0018 mL | 36.0036 mL |
| 5 mM | 720.1 μL | 3.6004 mL | 7.2007 mL |
| 10 mM | 360 μL | 1.8002 mL | 3.6004 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)