CAS |
No.69049-73-6 |
中文名称 |
多克罗 |
英文名称 |
Nedocromil |
分子式 |
C19H17NO7 |
分子量 |
371.34 |
溶解性 |
Soluble in DMSO ≥1mg/mL |
纯度 |
≥95% |
外观(性状) |
Light yellow to yellow Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
靶点 |
Others |
通路 |
Immunology & Inflammation |
背景说明 |
据报道,Nedocromil 抑制多种介质的作用或形成,包括组胺,白三烯 C4 (LTC4) 和前列腺素 D2 (PGD2)。 |
生物活性 |
Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).[1-2] |
In Vitro |
Nedocromil inhibits the release of histamine, LTC4, and PGD2 from mast cells challenged with antigen (with IC30 values of 2.1 μM, 2.3 μM, and 1.9 μM, respectively) and with anti-human IgE (IC30 values of 4.7 μM, 1.3 μM, and 1.3 μM, respectively)[1]. |
In Vivo |
Nedocromil-treated diabetic mice show significantly improved heart function compared with controls. The contractility and relaxation forces show similar improvements. However, the cardiac function of Nedocromil-treated diabetic mice remains significantly impaired when compared with normal mice. Nedocromil can significantly improve cardiac function in mice with diabetic cardiomyopathy, but the treatment cannot restore normal function[2]. |
动物实验 |
Mice[2]8-12 weeks old C57/BL6 male mice between 23-25 g receive intraperitoneal (i.p.) injections of 50 mg/kg Streptozotocin (STZ), dissolved in 100 mM citrate buffer pH 4.5, for five consecutive days. Diabetic mice (13-week-old) are randomly divided into three groups: 1) untreated group; 2) Nedocromil group, with Nedocromil released at the rate of 30 mg/kg per day from a subcutaneous (s.c.) pellet implantation; and vehicle group, with an inactive pellet implanted. Normal mice (non-diabetic) and normal mice that receive Nedocromil (30 mg/kg per day) are also included in this study for comparison. All sample groups included 15 mice (n=15)[2]. |
数据来源文献 |
[1]. Wells E, et al. Characterization of primate bronchoalveolar mast cells. II. Inhibition of histamine, LTC4, and PGD2 release from primate bronchoalveolar mast cells and a comparison with rat peritoneal mastcells. J Immunol. 1986 Dec 15;137(12):3941-5. [2]. Myocardial remodeling in diabetic cardiomyopathy associated with cardiac mast cell activation. Huang ZG, et al. PLoS One. 2013;8(3):e60827. |
规格 |
1mg 5mg 10mg 25mg 50mg |
单位 |
瓶 |