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- 详细信息
- 文献和实验
- 技术资料
- 库存:
43
- 英文名:
JNJ-7777120
- CAS号:
459168-41-3
- 供应商:
上海莼试
- 保存条件:
Store at -20°C
- 规格:
10mg 50mg
| 货号 | CS-01Y76640 | 规格 | 10mg 50mg |
| CAS号 | 459168-41-3 | 分子量 | 277.75 |
| 含量 | >99.50% | 别名 | |
| 分子式 | C14H16ClN3O | 化学名 | (5-chloro-1H-indol-2-yl)-(4-methylpiperazin-1-yl)methanone |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
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:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
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.
注意事项:
抗逆滴加序列
每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
反应时间及温度
加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
使用方法:
1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
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文献和实验Treatment of Infections Due to Resistant Staphylococcus aureus
, delafloxacin, and JNJ-Q2. Thus, there are currently many effective drugs to treat resistant S. aureus infections and many promising agents in the pipeline. Nevertheless, S. aureus remains a formidable adversary, and despite our deep bullpen of potential
Characterization of Histaminergic Receptors
H 4 Antagonists Thioperamide >100,000 >100,000 72.6 27 d Tocris Cookson JNJ7777140 c >10,000
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