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JNJ-7777120 98%

1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine

源叶(MedMol)
S27096
459168-41-3
C14H16ClN3O
277.75
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S27096-5mg 98% ¥400.00元 6 - - -
源叶(MedMol) S27096-10mg 98% ¥600.00元 5 - - -
源叶(MedMol) S27096-25mg 98% ¥1120.00元 6 - - -
源叶(MedMol) S27096-100mg 98% ¥3040.00元 预计交期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

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
产品描述: 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
靶点: H4 receptor;HistamineReceptor
体内研究:
JNJ-7777120 shows equipotent against the human, mouse, and rat receptors and exhibits at least 1000-fold selectivity over H1, H2, or H3 receptors. JNJ-7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ~3 h in both species. 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. JNJ-7777120 (10 mg/kg; s.c.; single) significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. Animal Model: BALB/c mice. Dosage: 20 mg/kg Administration: Subcutaneous injection; single daily for 2 days 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. Animal Model: Male outbred Swiss albino mice (zymosan-induced peritonitis model). Dosage: 10 mg/kg Administration: Subcutaneous injection; single Result: Led to a statistically significant reduction of neutrophil infiltration.
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. 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.
溶解性: Soluble  in  DMSO
保存条件: 2-8℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.6 ml 18.002 ml 36.004 ml
5 mM 0.72 ml 3.6 ml 7.201 ml
10 mM 0.36 ml 1.8 ml 3.6 ml
50 mM 0.072 ml 0.36 ml 0.72 ml
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参考文献

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