Molecular Weight(MW): 594.05
MK-3207 is a potent CGRP receptor antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2.
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(F) MK-3207 treatment led to a significant decrease of cAMP level (mean±SD, ***P＜0.001). (G) Embryos treated with MK-3207 showed no obvious T cell or HSPC defects.
Development, 2016, 143(12):2103-2110. . MK-3207 HCl purchased from Selleck.
(E) and (F) Nuclear factor κ-light-chain-enhancer of activated B cells (NF-κB) p65 and DNA binding assays. Synoviocytes were pretreated with L-703606 or MK-3207 for 2 hours, followed by 1 hour of stimulation with SP (100 nM) or CGRP (1 nM). *P < 0.05 versus control. #P < 0.05 versus synoviocytes stimulated with SP or CGRP alone.
Arthritis Res Ther, 2015.. MK-3207 HCl purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||MK-3207 is a potent CGRP receptor antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2.|
|Features||The most potent orally active CGRP receptor antagonist described to date.|
MK 3207 exhibits significantly higher affinity for both native and recombinant human CGRP receptor, as well as rhesus monkey CGRP receptor with Ki of 24 pM, ~24 pM and 22 pM, respectively, as compared to CGRP receptors from other species, including canine and rodent (Ki values of ~10 nM). Although has affinity for AMY1 (CTR/RAMP1) receptor with a Ki value of 0.75 nM, MK 3207 displays marked selectivity for human CGRP receptor versus related human AM1 (CLR/RAMP2) receptor, AM2 (CLR/RAMP3) receptor, AMY3 (CTR/RAMP3) receptor, and CTR with Ki values of 16.5 μM, 0.156 μM, 0.128 μM and 1.9 μM, respectively. MK 3207 potently inhibits human α-CGRP-induced cAMP production in HEK293 cells stably expressing human CLR/RAMP1 with an IC50 of 0.12 nM, and maintains similar potency in the presence of 50% human serum with an IC50 of 0.17 nM, indicating that the activity of MK 3207 would not be dramatically affected by plasma protein binding in vivo. MK 3207 exhibits approximately 65-fold more potent in the human serum-shifted in vitro functional assay than telcagepant with an IC50 of 10.9 nM. 
|In vivo||Administration of MK 3207 produces a concentration-dependent inhibition of capsaicin-induced dermal vasodilation in rhesus monkeys, blocking the blood flow increase with an EC50 of 0.8 nM and an EC90 of 7 nM, respectively. MK 3207 displays approximately 100-fold more potent in the rhesus monkey CIDV assay versus telcagepant with an EC90 of 994 nM. |
|In vitro||DMSO||119 mg/mL (200.31 mM)|
|Ethanol||119 mg/mL (200.31 mM)|
|Water||5 mg/mL (8.41 mM)|
|In vivo||1% DMSO+30% polyethylene glycol+1% Tween 80||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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