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MK-3207 Hydrochloride

CAS No. : 957116-20-0

MCE 站：MK-3207 Hydrochloride

产品活性：MK-3207 Hydrochloride 是一种有效的，可口服的 CGRP receptor 拮抗剂，IC₅₀ 值为 0.12 nM，K_i 值为 0.024 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：CGRP Receptor

In Vitro: MK-3207 displays a similar affinity (K_i) for the rhesus monkey receptor (0.024±0.001 nM; n=14) as for human, but it displays >400-fold lower affinity for the canine and rat receptors, with values of 10 nM and 10±1.2 nM, respectively. MK-3207 is highly selective versus the human AM1 (CLR/RAMP2) and AM2 (CLR/RAMP3) receptors, with K_i values of 16,500 nM and 156±17 nM, respectively. MK-3207 maintains a high degree of selectivity versus human CTR, with a K_i value of 1.9±0.58 μM. MK-3207 also displays good selectivity versus the AMY3 (CTR/RAMP3) receptor, with a K_i value of 128±25 nM, but it is less selective versus the AMY1 (CTR/RAMP1) receptor, with a K_i value of 0.75±0.13 nM. MK-3207 potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells, with an IC₅₀ value of 0.12±0.02 nM. MK-3207 displays significantly lower potency for the rat CGRP receptor, with a pIC₅₀=7.31±0.09.

In Vivo: MK-3207 is CNS-penetrant and therefore significantly engaging central receptors. After an oral dose of 10 mg/kg MK-3207, the CSF/plasma ratio is 2 to 3%.

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