| 溶解性 | 25°C: DMSO |
| 存贮条件 | 储存温度-20°C |
| 生化机理 | Description:IC50 Value: 0.024 nM (Ki, Human CGRP) [1]MK-3207 is a potent and orally bioavailable CGRP receptor antagonist. In common with other CGRP receptor antagonists, MK-3207 displays lower affinity for human CGRP receptors from other species, including canine and rodent.in vitro: MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM).in vivo: MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. The tritiated analog [3H]MK-3207 was used to study the binding characteristics on the human CGRP receptor. [3H]MK-3207 displayed reversible and saturable binding (K(D) = 0.06 nM), and the off-rate was determined to be 0.012 min(-1), with a t(1/2) value of 59 min [1]. After the first interim analysis, the two lowest MK-3207 doses (2.5, 5?mg) were identified as showing insufficient efficacy. Per the pre-specified adaptive design decision rule, only the 2.5-mg group was discontinued and the five highest doses (5, 10, 20, 50, 100?mg) were continued into the second stage [2].Clinical trial: MK-3207 for the treatment of acute migraines. Phase 2b |
MK-3207
MK-3207 （订货以英文为准）
编号：M127953
CAS号：957118-49-9
分子式：C31H29F2N5O3
分子量：557.59
| 货号 | 品牌 | 包装 | 目录价 | 您的价格 | 库存 | 数量 | 购买 |
|---|---|---|---|---|---|---|---|
| M127953-10mg | 阿拉丁 | 10mg | ¥3299.90 |
|
| 产品名称 | MK-3207 |
| 中文名称 | MK-3207 |
| CAS号 | 957118-49-9 |
| 分子式（M.F.） | C31H29F2N5O3 |
| 分子量（M.W.） | 557.59 |
| 储存条件 | -20°C储存 |
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