JNJ-7777120
目录号 : GC10400
Histamine H4 receptor antagonist
Cas No.:459168-41-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: A Histamine H4 receptor antagonist with IC50 of 4.5 nM.
Histamine has been reported to play an important role in a large number of physiological processes. JNJ-7777120, the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits more than 1000-fold selectivity over the other histamine receptors. [1]
In vitro: It was reported that NJ 7777120 bound to the H4 receptor with a remarkably high affinity. It also demonstrated a greater selectivity over other histamine receptor antagonists. Moreover, JNJ 7777120 selectively targeted to potent H4 rather than 50 other molecular targets. [2]
In vivo: JNJ 7777120 showed an oral bioavailability of about 30% in rats and 100% in dogs, with a half-life of around 3 h in both rats and dogs. It was reported to inhibit histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. In addition, in mice, JNJ 7777120 could suppress the histamine-induced migration of tracheal mast cells from the connective tissue to the epithelium. Moreover, JNJ 7777120 was demonstrated to notably inhibit neutrophil infiltration in a mouse zymosan-induced peritonitis model. [2]
Clinical trial: So far, no clinical trial has been conducted.
References:
[1]Jablonowski JA, Grice CA, Chai W, Dvorak CA, Venable JD, Kwok AK, Ly KS, Wei J, Baker SM, Desai PJ, Jiang W, Wilson SJ, Thurmond RL, Karlsson L, Edwards JP, Lovenberg TW and Carruthers NI. The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem. 2003 Sep; 46(19): 3957-60.
[2]Thurmond RL, Desai PJ, Dunford PJ, Fung-Leung WP, Hofstra CL, Jiang W, Nguyen S, Riley JP, Sun S, Williams KN, Edwards JP and Karlsson L. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004 Apr; 309(1): 404-13.
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。