产品说明
一般描述
A 1, 2, 4-triazole derived compound that acts as a potent ghrelin receptor (GHS-R1a) antagonist (IC50 = 32 nM in a binding assay, dissociation constant Kb = 19 nM). Shown to reduce hexarelin-induced food intake [hexarelin (80 µg/kg, cumulative food intake (g of food/100 g of body weight) at 6 h by acute administration (sc) of JMV 2959 (160 µg/kg)] in rats without affecting the basal food intake. Also suppresses ghrelin and fasting-induced food intake at the level of the central nervous system. Reported to suppress genes up-regulated by ghrelin. Does not affect intracellular Ca2+ mobilization.
包装
10 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Primary Target
Ghrelin receptor
警告
Toxicity: Standard Handling (A)
外形
Supplied as a hydrochloride salt.
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Moulin, A., et al. 2013. Amino Acids44, 301.
Mary, S., et al. 2012. Proc Natl Acad Sci USA109, 8304.
Salome, N., et al. 2009. Eur J Pharmacol.612, 167,.
Moulin, A., et al. 2007. J Med Chem50, 579.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C30H32N6O2 · xHCl |
| 分子量 | 508.61 (free base basis) |
产品性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | powder |
| 效能 | 32 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | beige |
| 溶解性 | DMSO: 100 mg/mL water: 5 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 2 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
