| 常用名 | MK-5046 | CAS号 | 1022152-70-0 |
|---|---|---|---|
| 价格 | ¥3474.0/5mg ¥需询单/1g ¥需询单/1g ¥需询单/1g | 纯度 | 99.0% |
| 备货期 | 1天 | 库存 | 现货 |
| 产品网页 | http://www.aladdin-e.com/zh_cn/M302090.html | ||
| 产品详情(用途,包装等)
用途: MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).IC50 value: 1.6 nM (Ki, for mouse), 25 nM (Ki, for human) [1]Target: BRS-3in vitro: MK-5046 is a novel BRS-3 agonist, with improved BRS-3 potency, specificity, and pharmacokinetic properties that allows in-depth investigation of BRS3 agonism in preclinical species and is also potentially suitable for use in humans. MK-5046 exhibits no appreciable binding activity at the neuromedin B and gastrin-releasing peptide receptors, as well as many other receptors, ion channels, and enzymes. In a cell-based Ca2+ mobilization functional assay, MK-5046 activates human BRS-3 with similar agonist efficacy as the peptide BRS-3 agonist.[1] MK-5046 is a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity.[2]in vivo: MK-5046 is the first BRS-3 agonist with properties suitable for use in larger mammals. In dogs, MK-5046 treatment produced statistically significant and persistent weight loss, which was initially accompanied by increases in body temperature and heart rate that abated with continued dosing. MK-5046 also effectively reduced body weight in rats and caused modest increases in body temperature, heart rate, and blood pressure. MK-5046 in rodents and dogs and further support BRS-3 agonism as a new approach to the treatment of obesity.[1] 物理化学性质: CAS号:1022152-70-0 常用中文名:MK-5046 常用英文名:MK-5046 分子式:C20H18F6N4O 分子量:444.37400 密度:N/A 沸点:N/A 熔点:N/A 闪点:N/A 储存条件:2-8℃ |