MK-3207
Cat. No. :YN320225
CAS No. :957118-49-9
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order@ubiochem.com| Product Name: | MK-3207 |
| CAS NO.: | 957118-49-9 |
| Chemical Name: | |
| Synonyms: | |
| Molecular Weight: | 557.59 |
| Molecular Formula: | C₃₁H₂₉F₂N₅O₃ |
| SMILES: | O=C1C2(NC[C@@H](C3=CC(F)=CC(F)=C3)N1CC(NC4=CC5=C(C[C@@]6(C(NC7=C6C=CC=N7)=O)C5)C=C4)=O)CCCC2 |
| Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Transportation: | Room temperature in continental US; may vary elsewhere. |
| Description: | MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12nM; Ki value= 0.024nM); highly selective versus human AM1, AM2, CTR, and AMY3. 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) = 0.024nM). in vivo: MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7nM 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) = 0.06nM), 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 . Clinical trial: MK-3207 for the treatment of acute migraines. Phase 2b |
| IC50&Target: | |
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