MK 3207
| CAS号 | 957118-49-9 | 货号 | BCP02225 |
| 中文名 | MK 3207 | ||
| 英文名 | MK 3207 | ||
| 中文别名 | |||
| 英文别名 | MK-3207;MK3207; | ||
| 分子式 | C31H29F2N5O3 | 分子量 | 557.59 |
| 生物活性 | 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. 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. | ||
| 信号通路 | Neuro Signaling Pathway GPCR/G Protein | ||
| 靶 点 | CGRP Receptor | ||
结构式
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