MK-8825
CAS No. : 1380887-60-4
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| Cat. No. : | HY-117694 |
| M.Wt: | 572.61 |
| Formula: | C31H30F2N6O3 |
| Purity: | >98 % |
| Solubility: |
MK-8825 is an orally active, selective CGRP receptor antagonist with a Ki value of 47 pM for human CGRP receptors and 17 nM for rat CGRP receptors. MK-8825 blocks CGRP-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders[1][2].
In Vitro:MK-8825 potently inhibits the binding of 125I-hCGRP to the native human CGRP receptor in SK-N-MC cells, with a Ki value of 0.052 nM[1].
MK-8825 potently inhibits the binding of 125I-hCGRP to rhesus monkey CGRP receptors, with a Ki value of 0.059 nM[1].
MK-8825 inhibits the binding of 125I-hCGRP to canine CGRP receptors, with a Ki value of 39 nM[1].
MK-8825 inhibits the binding of 125I-hCGRP to rabbit CGRP receptors, with a Ki value of 15 nM[1].
MK-8825 inhibits the binding of 125I-hCGRP to mouse CGRP receptors, with a Ki value of 19 nM[1].
MK-8825 potently blocks hCGRP-induced cAMP production in HEK293 cells expressing human CGRP receptors, with an IC50 of 0.23 nM[1].
MK-8825 inhibits the binding of human AM2 receptor with a Ki value of 590 nM[1].
MK-8825 inhibits the binding of human CT receptors with a Ki value of 3,200 nM[1].
MK-8825 inhibits the binding of human AMY1 receptor with a Ki value of 0.64 nM[1].
MK-8825 inhibits the binding of human AMY3 receptors with a Ki value of 1,100 nM[1].
In Vivo:MK-8825 (70 mg/kg; subcutaneous injection; single administration) significantly alleviates CFA (HY-153808)-induced acute orofacial nociceptive behaviors and trigeminal nucleus neuron activation in mice, without altering systemic IL-6 release[2].
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