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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
JNJ-7777120
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
459168-41-3
- 规格：
100mg/50mg/1mg/10mg/5mg
| 规格： | 100mg | 产品价格： | ￥4990.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥2990.0 |
| 规格： | 1mg | 产品价格： | ￥285.0 |
| 规格： | 10mg | 产品价格： | ￥1090.0 |
| 规格： | 5mg | 产品价格： | ￥640.0 |
| 基本信息 | |
| CAS | No.459168-41-3 |
| 英文名称 | JNJ-7777120 |
| 别名 | (5-氯-1H-吲哚-2-基)(4-甲基哌嗪-1-基)甲酮 |
| 分子式 | C14H16ClN3O |
| 分子量 | 277.75 |
| 溶解性 | Soluble in DMSO(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD04343337 |
| SMILES | CN1CCN(CC1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl |
| InChIKey | HUQJRYMLJBBEDO-UHFFFAOYSA-N |
| InChI | InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3，8-9，16H，4-7H2，1H3 |
| PubChem CID | 4908365 |
| 靶点 | Histamine H4 Receptor |
| 通路 | GPCR & G Protein;Neuronal Signaling;Immunology & Inflammation |
| 背景说明 | 是一种选择性的组胺H4受体拮抗剂。 |
| 生物活性 | JNJ-7777120 是一种选择性组胺 H4 受体拮抗剂，其Ki值为4.5 nM，具有抗瘙痒和抗炎活性。[1-2] |
| In Vitro | JNJ 7777120 has a K(i)of 4.5 nM versus the human histamine H4 receptor and a pA(2)of 8.1. JNJ 7777120(10 μM)blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells.[1] JNJ7777120 inhibited dose-dependently the production of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 from antigen-stimulated BMMC.[2] |
| 细胞实验 | JNJ 7777120 is equipotent against the human，mouse，and rat receptors. It exhibits at least 1000-fold selectivity over H1，H2，or H3 receptors. JNJ 7777120 has an oral bioavailability of approximately 30% in rats and 100% in dogs，with a half-life of approximately 3 h in both species. JNJ 7777120(20mg/kg; s.c.)blocks the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ 7777120(10mg/kg; s.c.)significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model.[1] Combined treatment with H1R antagonist olopatadine and H4R antagonist JNJ777712 may have a significant therapeutic effect on chronic dermatitis.[2] |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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IJ0250 JNJ-7777120 抑制剂/拮抗剂/激动剂 索莱宝
￥285 - 4990
