JNJ-7777120
Based on 1 publication(s) in Google Scholar
JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.95%
- CAS 番号: 459168-41-3
- 分子式: C14H16ClN3O
- 分子量:277.75
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 JNJ-7777120
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生物活性
製品説明
IC50 & Target
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H4 receptor |
体外実験
JNJ-7777120 (0, 10, 100, 1000 nM; ~6 h) shows functional antagonism of the human and mouse histamine H4 receptors in SK-N-MC cells[1].
JNJ-7777120 (10 μM; 10 min) blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells[1].
JNJ7777120 (30-100 μM; 30 min) inhibits dose-dependently the production of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 from antigen-stimulated BMMC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-N-MC cells (expressing the human or mouse histamine H4 receptor)
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Concentration:0, 10, 100, 1000 nM
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Incubation Time:~6 h
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Result:Exhibited antagonistic effect on human and mouse histamine H4 receptors.
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Cell Line:Mouse mast cells
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Concentration:10 µM
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Incubation Time:10 min
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Result:Exhibited a very potent antagonistic effect on the H4 receptor in primary cells.
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Cell Line:BMMC
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Concentration:30-100 µM
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Incubation Time:30 min
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Result:Significantly inhibited the production of TARC (thymus and activation-regulated chemokine) and MDC (macrophage-derived chemokine).
体内実験
JNJ-7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ~3 h in both species[1].
JNJ-7777120 (20 mg/kg; s.c.; single daily for 2 days) blocks the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice[1].
JNJ-7777120 (10 mg/kg; s.c.; single) significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice[1].
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Dosage:20 mg/kg
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Administration:Subcutaneous injection; single daily for 2 days
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Result:Blocked histamine induced an increase in the number of mast cells per tracheal section and a significant migration of mast cells towards the tracheal epithelium.
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Animal Model:Male outbred Swiss albino mice (zymosan-induced peritonitis model)[1].
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Dosage:10 mg/kg
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Administration:Subcutaneous injection; single
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Result:Led to a statistically significant reduction of neutrophil infiltration.
化学情報
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CAS 番号 459168-41-3
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性状 Solid
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分子量 277.75
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分子式 C14H16ClN3O
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Color White to off-white
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SMILES
O=C(C(N1)=CC2=C1C=CC(Cl)=C2)N3CCN(C)CC3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Pain
Histamine H4 receptor and TRPV1 mediate itch induced by cadaverine, a metabolite of the microbiome. [Abstract]2024 Jan-Dec:20:17448069241272149. PMID: 39079948
溶剤 & 溶解度
体外:
DMSO : ≥ 50 mg/mL (180.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Thurmond RL, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004 Apr;309(1):404-13. [Content Brief]
[2]. Ohsawa Y, et al. The antagonism of histamine H1 and H4 receptors ameliorates chronic allergic dermatitis via anti-pruritic and anti-inflammatory effects in NC/Nga mice. Allergy. 2012 Aug;67(8):1014-22. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6004 mL | 18.0018 mL | 36.0036 mL | 90.0090 mL |
| 5 mM | 0.7201 mL | 3.6004 mL | 7.2007 mL | 18.0018 mL | |
| 10 mM | 0.3600 mL | 1.8002 mL | 3.6004 mL | 9.0009 mL | |
| 15 mM | 0.2400 mL | 1.2001 mL | 2.4002 mL | 6.0006 mL | |
| 20 mM | 0.1800 mL | 0.9001 mL | 1.8002 mL | 4.5005 mL | |
| 25 mM | 0.1440 mL | 0.7201 mL | 1.4401 mL | 3.6004 mL | |
| 30 mM | 0.1200 mL | 0.6001 mL | 1.2001 mL | 3.0003 mL | |
| 40 mM | 0.0900 mL | 0.4500 mL | 0.9001 mL | 2.2502 mL | |
| 50 mM | 0.0720 mL | 0.3600 mL | 0.7201 mL | 1.8002 mL | |
| 60 mM | 0.0600 mL | 0.3000 mL | 0.6001 mL | 1.5002 mL | |
| 80 mM | 0.0450 mL | 0.2250 mL | 0.4500 mL | 1.1251 mL | |
| 100 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL | 0.9001 mL |
JNJ-7777120 関連分類
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